HIF-1a

Hypoxia-inducible factor 1-alpha

Reviewed UniProt entries for HIF-1a and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
Q0PGG7 HIF1A_BOSMU Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) HIF1A Bos mutus grunniens (Wild yak) (Bos grunniens) 823
Q9XTA5 HIF1A_BOVIN Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) HIF1A Bos taurus (Bovine) 823
Q9YIB9 HIF1A_CHICK Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) HIF1A Gallus gallus (Chicken) 811
Q309Z6 HIF1A_EOSBA Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) HIF1A Eospalax baileyi (Plateau zokor) (Myospalax baileyi) 819
Q61221 HIF1A_MOUSE Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) (ARNT-interacting protein) Hif1a Mus musculus (Mouse) 836
Q98SW2 HIF1A_ONCMY Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) hif1a Oncorhynchus mykiss (Rainbow trout) (Salmo gairdneri) 766
O35800 HIF1A_RAT Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) Hif1a Rattus norvegicus (Rat) 825
Q9I8A9 HIF1A_XENLA Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) hif1a Xenopus laevis (African clawed frog) 805
Q16665 HIF1A_HUMAN Hypoxia-inducible factor 1-alpha (HIF-1-alpha) (HIF1-alpha) (ARNT-interacting protein) (Basic-helix-loop-helix-PAS protein MOP1) (Class E basic helix-loop-helix protein 78) (bHLHe78) (Member of PAS protein 1) (PAS domain-containing protein 8) HIF1A BHLHE78 MOP1 PASD8 Homo sapiens (Human) 826

Small molecules tested in HIF-1a binding assays:

437 datapoints for 252 distinct small molecules


Name CHEMBL1077108
Affinity Not Active
Assay description Inhibition of hypoxia-induced nuclear HIF1alpha in human T47D cells at 30 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18989978
Doc title Molecular-targeted antitumor agents. 19. Furospongolide from a marine Lendenfeldia sp. sponge inhibits hypoxia-inducible factor-1 activation in breast tumor cells.
PDB None

Name CHEMBL1077108
Affinity Active
Assay description Inhibition of hypoxia-induced nuclear HIF1alpha in human T47D cells at 10 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18989978
Doc title Molecular-targeted antitumor agents. 19. Furospongolide from a marine Lendenfeldia sp. sponge inhibits hypoxia-inducible factor-1 activation in breast tumor cells.
PDB None

Name CHEMBL1077108
Affinity Not Active
Assay description Inhibition of 1,10-phenanthroline-induced nuclear HIF1alpha in human T47D cells at 10 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18989978
Doc title Molecular-targeted antitumor agents. 19. Furospongolide from a marine Lendenfeldia sp. sponge inhibits hypoxia-inducible factor-1 activation in breast tumor cells.
PDB None

Name CHEMBL1089316
Affinity IC50 = 0.1uM
Assay description Inhibition of HIF-1alpha-mediated VEGF secretion in human Hep3b cells by ELISA
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22305612
Doc title Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PDB None

Name CHEMBL1089316
Affinity IC50 = 12.5uM
Assay description Inhibition of HIF-1alpha transcriptional co-activator p300 interaction
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22305612
Doc title Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PDB None

Name CHEMBL1089316
Affinity IC50 = 0.04uM
Assay description Inhibition of HIF-1alpha-mediated VEGF expression in human Hep3b cells by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22305612
Doc title Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PDB None

Name CHEMBL109480
Affinity Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 0.4 uM after 12 hrs by dual luciferase reporter gene assay in presence of dipyridol
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL109480
Affinity Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 0.4 uM after 12 hrs by dual luciferase reporter gene assay in absence of dipyridol
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL123292
Affinity Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human T47D cells at 10 uM after 4 hrs by Western blotting
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15974627
Doc title Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
PDB None

Name CHEMBL123292
Affinity Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human T47D cells at 0.3 uM after 4 hrs by Western blotting
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15974627
Doc title Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
PDB None

Name CHEMBL123292
Affinity Active
Assay description Inhibition of 1,10-phenanthroline-induced HIF1alpha activation in human T47D cells at 10 uM after 4 hrs by Western blotting
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15974627
Doc title Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
PDB None

Name CHEMBL123292
Affinity Active
Assay description Inhibition of 1,10-phenanthroline-induced HIF1alpha activation in human T47D cells at 0.3 uM after 4 hrs by Western blotting
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15974627
Doc title Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
PDB None

Name CHEMBL1269016
Affinity IC50 = 6uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269016
Affinity IC50 = 2uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269329
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269394
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269395
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269396
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269397
Affinity IC50 = 22uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269397
Affinity IC50 = 6uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269422
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269423
Affinity IC50 = 5.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269424
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269467
Affinity IC50 = 1.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269467
Affinity IC50 = 5.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269468
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269484
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269485
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1269486
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271811
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271866
Affinity IC50 = 8uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271866
Affinity IC50 = 0.8uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271866
Affinity Dose-dependent effect
Assay description Inhibition of HIF1-alpha-mediated VEGF mRNA expression in human PC3 cells under hypoxic condition by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271867
Affinity IC50 = 5.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271867
Affinity IC50 = 1.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271868
Affinity IC50 = 10uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271868
Affinity IC50 = 4uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271922
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271923
Affinity IC50 > 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271924
Affinity IC50 = 1.8uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271924
Affinity IC50 = 22uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271978
Affinity IC50 = 2uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271978
Affinity IC50 = 30uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271979
Affinity IC50 = 3.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271979
Affinity IC50 = 15uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271980
Affinity IC50 = 1.5uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1271980
Affinity IC50 = 8uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1272036
Affinity IC50 = 8uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1272037
Affinity IC50 = 10uM
Assay description Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1272037
Affinity IC50 = 1.4uM
Assay description Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932758
Doc title Development of novel inhibitors targeting HIF-1alpha towards anticancer drug discovery.
PDB None

Name CHEMBL1342148
Affinity EC50 = 8.85uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1345388
Affinity EC50 = 4.62uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1345388
Affinity EC50 = 6.15uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1345388
Affinity EC50 = 7.13uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1345685
Affinity IC50 = 0.43uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1451745
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1458314
Affinity EC50 = 8.67uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1458314
Affinity EC50 = 15.8uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1458314
Affinity EC50 = 7.72uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1505546
Affinity EC50 = 20uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1505546
Affinity EC50 = 28uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1505546
Affinity EC50 = 23.9uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL153
Affinity Not Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL1560590
Affinity EC50 = 9.82uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1560590
Affinity EC50 = 7.46uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL1560590
Affinity EC50 = 9.06uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL157844
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL157844
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL1782072
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1782072
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1782072
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1782072
Affinity IC50 = 7.21uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783622
Affinity IC50 = 32.7uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783623
Affinity IC50 = 69.9uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783624
Affinity IC50 = 35.5uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783625
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783625
Affinity IC50 = 17.4uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783625
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783626
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783626
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783626
Affinity IC50 = 52.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783627
Affinity IC50 = 23uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783628
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783628
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783628
Affinity IC50 = 51.7uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783629
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783629
Affinity IC50 = 41.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783629
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783630
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783630
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783630
Affinity IC50 > 100uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783631
Affinity IC50 = 32.5uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783631
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783631
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783632
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783632
Affinity IC50 > 100uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783632
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783633
Affinity IC50 = 39.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783634
Affinity IC50 = 18.7uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783635
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783635
Affinity IC50 = 8.62uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783635
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783636
Affinity IC50 = 29.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783637
Affinity IC50 = 22.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1783638
Affinity IC50 = 15.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1795426
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795427
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795428
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795429
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795430
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795431
Affinity IC50 = 5.3uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795432
Affinity IC50 = 6.76nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795433
Affinity IC50 = 10nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795434
Affinity IC50 = 46nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795435
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha-mediated VEGF production in human Hep3B cells under hypoxic condition after 17.5 hrs by ELISA
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795435
Affinity IC50 = 4.2nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795436
Affinity IC50 = 54nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795437
Affinity IC50 = 490nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795438
Affinity IC50 = 580nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795439
Affinity IC50 = 7nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795440
Affinity IC50 = 110nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795441
Affinity IC50 = 54nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795442
Affinity IC50 = 310nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795443
Affinity IC50 = 360nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795444
Affinity IC50 = 1100nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795445
Affinity IC50 > 30nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795446
Affinity IC50 = 1nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795447
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795448
Affinity IC50 = 26.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795449
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795450
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795451
Affinity IC50 = 17.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795452
Affinity IC50 = 17.5uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795453
Affinity IC50 = 17.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795454
Affinity IC50 = 16.8uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795455
Affinity IC50 = 7.3uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795456
Affinity IC50 = 2.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1795457
Affinity IC50 = 12.9uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL1833996
Affinity IC50 = 27.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836173
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836174
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836175
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836176
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836177
Affinity IC50 = 3.3uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836178
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836179
Affinity IC50 = 0.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836180
Affinity IC50 = 4.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836181
Affinity IC50 = 4.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836182
Affinity IC50 = 22.9uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836183
Affinity IC50 = 6.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836184
Affinity IC50 = 3.5uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836185
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836229
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836230
Affinity IC50 = 1.2uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836231
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836232
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836233
Affinity IC50 = 0.47uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836234
Affinity IC50 = 1.7uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836235
Affinity IC50 = 9.4uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836236
Affinity IC50 = 0.81uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836237
Affinity IC50 = 27.5uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836238
Affinity IC50 = 0.09uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836239
Affinity IC50 = 0.16uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836240
Affinity IC50 = 27.6uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836241
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836242
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836243
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836244
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1836245
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21831635
Doc title Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL1928022
Affinity Dose-dependent effect
Assay description Inhibition of hypoxia-induced HIF1alpha protein reduction in human Hep3B cells by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21937231
Doc title Design, synthesis and insight into the structure-activity relationship of 1,3-disubstituted indazoles as novel HIF-1 inhibitors.
PDB None

Name CHEMBL198075
Affinity Dose-dependent effect
Assay description Inhibition of hypoxia-induced HIF1alpha protein accumulation in human AGS cells after 12 hrs by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16872154
Doc title Phenanthroquinolizidine alkaloids from the roots of Boehmeria pannosa potently inhibit hypoxia-inducible factor-1 in AGS human gastric cancer cells.
PDB None

Name CHEMBL2021443
Affinity IC50 = 47nM
Assay description Inhibition of CoCl2-induced HIF1alpha expression in mouse 4T1 cells transfected with oxygen-dependent-degradation domain of HIFalpha by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19423348
Doc title Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.
PDB None

Name CHEMBL2021447
Affinity Not Active
Assay description Inhibition of CoCl2-induced HIF1alpha expression in mouse 4T1 cells transfected with oxygen-dependent-degradation domain of HIFalpha by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19423348
Doc title Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.
PDB None

Name CHEMBL2057226
Affinity Not Active
Assay description Effect on stabilization of HIF-1alpha in deferoxamine treated human HeLa cells at 50 to 500 uM by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22789427
Doc title Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1alpha-p300 interaction by a small molecule.
PDB None

Name CHEMBL2057226
Affinity Active
Assay description Inhibition of HIF-1alpha in deferoxamine treated human HeLa cells assessed as reduction of VEGF mRNA level at 100 uM after 5 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22789427
Doc title Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1alpha-p300 interaction by a small molecule.
PDB None

Name CHEMBL205924
Affinity IC50 = 6.76nM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21481991
Doc title HIF-1alpha inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.
PDB None

Name CHEMBL2069708
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha in human U2OS cells in normaxia condition
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22889802
Doc title A novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines.
PDB None

Name CHEMBL2069708
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha in human U2OS cells in hypoxia condition
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22889802
Doc title A novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines.
PDB None

Name CHEMBL2130568
Affinity EC50 = 3.45uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2130568
Affinity EC50 = 4.74uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2130568
Affinity EC50 = 2.46uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2130848
Affinity EC50 = 8.72uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2130848
Affinity EC50 = 3.63uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2130848
Affinity EC50 = 9.82uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131608
Affinity EC50 = 22.9uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131608
Affinity EC50 = 11.6uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131608
Affinity EC50 = 12.1uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131991
Affinity EC50 = 4.74uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131991
Affinity EC50 = 3.67uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2131991
Affinity EC50 = 3.73uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2132069
Affinity EC50 = 6.73uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2132069
Affinity EC50 = 1.88uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2132069
Affinity EC50 = 1.2uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134094
Affinity EC50 = 6.67uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134094
Affinity EC50 = 9.54uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134094
Affinity EC50 = 3.08uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134352
Affinity EC50 = 9.84uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134352
Affinity EC50 = 9.6uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2134352
Affinity EC50 = 17.5uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2135309
Affinity EC50 = 0.5uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2135309
Affinity EC50 = 2.57uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2135309
Affinity EC50 = 2.49uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2136245
Affinity EC50 = 27.8uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2136245
Affinity EC50 = 6.45uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2136245
Affinity EC50 = 7.62uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2137226
Affinity EC50 = 1.49uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2137226
Affinity EC50 = 2.33uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2137226
Affinity EC50 = 2.77uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2138065
Affinity EC50 = 0.6uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2138065
Affinity EC50 = 1.71uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2138065
Affinity EC50 = 1.12uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139663
Affinity EC50 = 1.19uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139663
Affinity EC50 = 2.6uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139663
Affinity EC50 = 4.58uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139973
Affinity EC50 = 2.39uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139973
Affinity EC50 = 2.91uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2139973
Affinity EC50 = 5.41uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140244
Affinity EC50 = 6.27uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140244
Affinity EC50 = 4.15uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140244
Affinity EC50 = 3.92uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140280
Affinity EC50 = 10.6uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140280
Affinity EC50 = 25uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140280
Affinity EC50 = 10.5uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140836
Affinity EC50 = 8.38uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140836
Affinity EC50 = 29.5uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2140836
Affinity EC50 = 7.67uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141631
Affinity EC50 = 4.46uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141631
Affinity EC50 = 3.26uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141631
Affinity EC50 = 7.64uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141722
Affinity EC50 = 2.48uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141722
Affinity EC50 = 3.82uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141722
Affinity EC50 = 2.97uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141772
Affinity EC50 = 4.27uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141772
Affinity EC50 = 6.21uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2141772
Affinity EC50 = 12.7uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2142554
Affinity EC50 = 1.85uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2142554
Affinity EC50 = 2.96uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2142554
Affinity EC50 = 2.3uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144203
Affinity EC50 = 2.06uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144203
Affinity EC50 = 2.55uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144203
Affinity EC50 = 4.17uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144958
Affinity EC50 = 5.01uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM zinc
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144958
Affinity EC50 = 1.63uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144958
Affinity EC50 = 1.4uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144958
Affinity EC50 = 1.12uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2144958
Affinity EC50 = 15.6uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM iron
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152027
Affinity EC50 = 22uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152027
Affinity EC50 = 3.04uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152027
Affinity EC50 = 7.57uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152028
Affinity EC50 = 24.9uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152028
Affinity EC50 = 16.6uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152028
Affinity EC50 = 21.5uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152029
Affinity EC50 = 10uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152029
Affinity EC50 = 20.8uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152029
Affinity EC50 = 9.08uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152030
Affinity EC50 = 14.2uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152030
Affinity EC50 = 8.12uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152030
Affinity EC50 = 6.27uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152031
Affinity EC50 = 10.2uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152031
Affinity EC50 = 21.9uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152031
Affinity EC50 = 8.69uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152032
Affinity EC50 = 5.41uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152032
Affinity EC50 = 7.55uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152032
Affinity EC50 = 22.4uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152106
Affinity EC50 = 26uM
Assay description Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152106
Affinity EC50 = 5.02uM
Assay description Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152106
Affinity EC50 = 4.35uM
Assay description Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22172704
Doc title Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
PDB None

Name CHEMBL2152288
Affinity Active
Assay description Inhibition of HIF1alpha-mediated VEGF production in human MCF7 cells under hypoxic condition at 0.1 to 10 uM after 6 hrs
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22575050
Doc title Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities.
PDB None

Name CHEMBL2177118
Affinity IC50 = 2.54uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2177347
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase 9 expression after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177347
Affinity Not Active
Assay description Inhibition of HIF1alpha in human RCC4 cells coexpressing HIF2alpha assessed as decrease in carbonic anhydrase 9 mRNA expression after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177347
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177348
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase expression at 79 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177348
Affinity Active
Assay description Inhibition of HIF1alpha in human RCC4 cells coexpressing HIF2alpha assessed as decrease in carbonic anhydrase 9 mRNA expression at 79 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177348
Affinity Not Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA expression at 79 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177349
Affinity Active
Assay description Inhibition of HIF1alpha in human RCC4 cells coexpressing HIF2alpha assessed as decrease in carbonic anhydrase 9 mRNA expression at 21 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177349
Affinity Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA expression at 21 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177349
Affinity Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase 9 expression at 21 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177350
Affinity Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase 9 expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177350
Affinity Active
Assay description Inhibition of HIF1alpha in human RCC4 cells coexpressing HIF2alpha assessed as decrease in carbonic anhydrase 9 mRNA expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177350
Affinity Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2177350
Affinity Active
Assay description Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA expression at 20 uM after 48 hrs by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22928967
Doc title Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
PDB None

Name CHEMBL2178399
Affinity Not Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 5 uM after 12 hrs by dual luciferase reporter gene assay in presence of dipyridol
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity IC50 = 0.12uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition assessed as decrease in EPO mRNA expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition assessed as increase in VHL expression at 2 to 5 uM by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under normoxic condition assessed as increase in VHL expression at 2 to 5 uM by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition assessed as decrease in VEGF mRNA expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Active
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 5 uM after 12 hrs by dual luciferase reporter gene assay in absence of dipyridol
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178399
Affinity Dose-dependent effect
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition assessed as decrease in MMP9 mRNA expression by RT-PCR analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178400
Affinity IC50 > 20uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178401
Affinity IC50 > 20uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178402
Affinity IC50 > 20uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178403
Affinity IC50 = 1.34uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178404
Affinity IC50 = 1.07uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178405
Affinity IC50 = 1.85uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178406
Affinity IC50 = 15.75uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178407
Affinity IC50 = 0.74uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178408
Affinity IC50 = 6.03uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178409
Affinity IC50 = 1.04uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178410
Affinity IC50 = 2.17uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178411
Affinity IC50 = 4.12uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178412
Affinity IC50 > 20uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178413
Affinity IC50 > 20uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178414
Affinity IC50 = 1.18uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178415
Affinity IC50 = 2.38uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178416
Affinity IC50 = 0.82uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178417
Affinity IC50 = 1.84uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178418
Affinity IC50 = 2.62uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL2178419
Affinity IC50 = 1.35uM
Assay description Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23153200
Doc title Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1alpha inhibitors.
PDB None

Name CHEMBL219673
Affinity IC50 = 0.4uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL219673
Affinity IC50 = 0.35uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL2205733
Affinity IC50 = 7.5uM
Assay description Inhibition of HIF-1alpha in human LN229 cells under hypoxia condition by HRE-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22305612
Doc title Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PDB None

Name CHEMBL2205734
Affinity IC50 = 0.003uM
Assay description Inhibition of HIF-1alpha in human HCT116 cells under hypoxia condition by HRE-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22305612
Doc title Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PDB None

Name CHEMBL223862
Affinity IC50 = 3.1uM
Assay description Inhibition of hypoxia-induced HIF1alpha activation in human HeLa cells after 12 hrs by HRE-luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20083404
Doc title Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL235553
Affinity Not Active
Assay description Inhibition of hypoxia-induced HIF1 activation in humanT47D cells at 30 uM after 16 hrs by cell based luciferase assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18004798
Doc title Total synthesis and absolute configuration of laurenditerpenol: a hypoxia inducible factor-1 activation inhibitor.
PDB None

Name CHEMBL235553
Affinity IC50 = 0.82uM
Assay description Inhibition of hypoxia-induced HIF1 activation in human T47D cells after 16 hrs by cell based luciferase assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18004798
Doc title Total synthesis and absolute configuration of laurenditerpenol: a hypoxia inducible factor-1 activation inhibitor.
PDB None

Name CHEMBL236799
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia-induced HIF1 activation in human T47D cells after 16 hrs by cell based luciferase assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18004798
Doc title Total synthesis and absolute configuration of laurenditerpenol: a hypoxia inducible factor-1 activation inhibitor.
PDB None

Name CHEMBL248650
Affinity IC50 = 4.1uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248650
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248650
Affinity IC50 = 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248835
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248835
Affinity IC50 = 18.6uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248835
Affinity IC50 = 2.5uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248836
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248836
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL248836
Affinity IC50 = 1.3uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249023
Affinity IC50 = 3.4uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249023
Affinity IC50 = 3.4uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249023
Affinity IC50 = 5.2uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249027
Affinity IC50 = 3.1uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249027
Affinity IC50 = 1.8uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249027
Affinity IC50 = 0.6uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249028
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249028
Affinity IC50 = 5uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL249028
Affinity IC50 = 5.9uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL250671
Affinity IC50 = 1.9uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL250671
Affinity IC50 > 10uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL250671
Affinity IC50 > 10uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL254799
Affinity Not Active
Assay description Inhibition of HIF1alpha
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18501601
Doc title Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
PDB None

Name CHEMBL255001
Affinity Not Active
Assay description Inhibition of HIF1alpha
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18501601
Doc title Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
PDB None

Name CHEMBL257371
Affinity Active
Assay description Inhibition of HIF1alpha
-- Homologous single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18501601
Doc title Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.
PDB None

Name CHEMBL333985
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL333985
Affinity IC50 = 2uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL333985
Affinity IC50 = 9.21uM
Assay description Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL333985
Affinity Active
Assay description Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19435661
Doc title 1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
PDB None

Name CHEMBL333985
Affinity IC50 = 13.8uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL333985
Affinity IC50 > 30uM
Assay description Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17884495
Doc title Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
PDB None

Name CHEMBL36327
Affinity Not Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis in presence of 300 uM iron(2)
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Not Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis in presence of 150 uM iron(3)
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Active
Assay description Inhibition of hypoxia-induced increase in HIF1alpha protein in human T47D cells at 100 uM after 4 hrs by Western blot analysis
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Not Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis in presence of ascorbate
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Not Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis in presence of 100 uM iron(2)
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None

Name CHEMBL36327
Affinity Active
Assay description Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis in presence of trolox
-- Direct single protein target assigned: HIF1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15620252
Doc title Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
PDB None