Rac1

Ras-related c3 botulinum toxin substrate 1

Reviewed UniProt entries for Rac1 and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
Q6RUV5 RAC1_RAT Ras-related C3 botulinum toxin substrate 1 (p21-Rac1) Rac1 Rattus norvegicus (Rat) 192
P62998 RAC1_BOVIN Ras-related C3 botulinum toxin substrate 1 (p21-Rac1) RAC1 Bos taurus (Bovine) 192
P62999 RAC1_CANFA Ras-related C3 botulinum toxin substrate 1 (Rac2) (p21-Rac1) RAC1 Canis familiaris (Dog) (Canis lupus familiaris) 192
P80236 RAC1_CAVPO Ras-related C3 botulinum toxin substrate 1 (Sigma 1 component protein p22) (p21-Rac1) (Fragment) RAC1 Cavia porcellus (Guinea pig) 77
P63000 RAC1_HUMAN Ras-related C3 botulinum toxin substrate 1 (Cell migration-inducing gene 5 protein) (Ras-like protein TC25) (p21-Rac1) RAC1 TC25 MIG5 Homo sapiens (Human) 192
P63001 RAC1_MOUSE Ras-related C3 botulinum toxin substrate 1 (p21-Rac1) Rac1 Mus musculus (Mouse) 192

Small molecules tested in Rac1 binding assays:

118 datapoints for 76 distinct small molecules


Name CHEMBL12089
Affinity INH = 14%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL257119
Affinity INH = 88.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL257119
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 100 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL257119
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL258893
Affinity IC50 > 100uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL258893
Affinity INH = 49%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL274189
Affinity INH = 15%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Effect on Rac1 binding to RhoGDI2 expressed in 293T cells by Western blot analysis
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Effect on Rac1 binding to RhoGDI1 expressed in 293T cells by Western blot analysis
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Binding affinity at Rac1 at 1 uM by fluorescence anisotropy
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity INH = 100%
Assay description Inhibition of Rac1-PAK-RBD complex formation in platelet derived growth factor-induced human U87MG cells at 50 uM by fluorescence anisotropy
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Effect on Rac1 binding to RhoGDI2 in mouse NIH3T3 cells by Western blot analysis
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Effect on Rac1 binding to RhoGDI1 in mouse NIH3T3 cells by Western blot analysis
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Dose-dependent effect
Assay description Inhibition of platelet derived growth factor-induced endogenous association of Rac1 with GST-PAK-RBD in human U87MG cells after 5 mins by Western blot analysis
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Binding affinity to Rac1 at 1 uM by fluorescence anisotropy
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Binding affinity at Rac1b at 1 uM by fluorescence anisotropy
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Dose-dependent effect
Assay description Inhibition of EDTA-induced nucleotide exchange on Rac1-mant-GDP by FRET assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL470891
Affinity Active
Assay description Inhibition of Tiam1-induced nucleotide exchange on Rac1-mant-GDP by FRET assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17932039
Doc title Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.
PDB None

Name CHEMBL490129
Affinity IC50 = 58uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL490129
Affinity INH = 63%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL549323
Affinity INH = 76%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL549401
Affinity INH = 98.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL549739
Affinity INH = 121.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL549943
Affinity INH = 72.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL550079
Affinity INH = 76.1%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL550826
Affinity IC50 = 46.1uM
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level after 4 hrs by G-LISA
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL550826
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 levels at 25 uM after 4 hrs by pull-down assay
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL550826
Affinity INH = 52%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL551233
Affinity INH = 78.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL551431
Affinity INH = 89.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL551492
Affinity INH = 77.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL552035
Affinity INH = 87.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL552501
Affinity INH = 83.1%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL552502
Affinity INH = 83.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL554475
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 levels at 25 uM after 4 hrs by pull-down assay
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL554475
Affinity IC50 = 28.3uM
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level after 4 hrs by G-LISA
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL554475
Affinity INH = 50.3%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL554922
Affinity INH = 68.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL555870
Affinity INH = 96.5%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL557208
Affinity INH = 58.5%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL557275
Affinity INH = 94.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558282
Affinity INH = 70.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558283
Affinity INH = 83.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1-mediated cellular events in mouse 3T3 cells assessed as induction of membrane lamillipodia at 25 uM after 48 hrs by fluorescent microscopy
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Activity = -86%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 levels at 25 uM after 4 hrs by pull-down assay
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity assessed as blockade of Rac1-Tiam1 interaction in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity IC50 = 12.2uM
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level after 4 hrs by G-LISA
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1-mediated cellular events in mouse 3T3 cells assessed as induction of membrane ruffling formation at 25 uM after 48 hrs by fluorescent microscopy
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 100 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558673
Affinity INH = 54.2%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558676
Affinity INH = 61.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558677
Affinity INH = 65.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL558878
Affinity INH = 67.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559432
Affinity INH = 72.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559630
Affinity INH = 110.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559632
Affinity INH = 97.1%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559640
Affinity INH = 68.6%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559901
Affinity INH = 80.3%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL559959
Affinity INH = 83.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL560355
Affinity INH = 85.5%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL560757
Affinity INH = 72.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561018
Affinity INH = 98.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561026
Affinity INH = 95.2%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561218
Affinity INH = 131.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561297
Affinity INH = 109.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561759
Affinity INH = 74.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL561836
Affinity INH = 86.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity IC50 = 24.1uM
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level after 4 hrs by G-LISA
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 levels at 25 uM after 4 hrs by pull-down assay
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1-mediated cellular events in mouse 3T3 cells assessed as induction of membrane lamillipodia at 25 uM after 48 hrs by fluorescent microscopy
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1-mediated cellular events in mouse 3T3 cells assessed as induction of membrane ruffling formation at 25 uM after 48 hrs by fluorescent microscopy
-- Direct single protein target assigned: RAC1_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity assessed as blockade of Rac1-Tiam1 interaction in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity Active
Assay description Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 100 uM by SDS-PAGE based chemiluminescence
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562095
Affinity INH = 34.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562294
Affinity INH = 84.6%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL562579
Affinity INH = 69.1%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563017
Affinity INH = 118%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563045
Affinity INH = 62.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563222
Affinity INH = 90.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563777
Affinity INH = 54.8%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563777
Affinity Active
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of ratio of Rac1GTP/Rac1 levels at 25 uM after 4 hrs by pull-down assay
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL563777
Affinity IC50 = 57.2uM
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level after 4 hrs by G-LISA
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL564693
Affinity INH = 62.2%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL564830
Affinity INH = 130.9%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL565118
Affinity INH = 68%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL565215
Affinity INH = 104.7%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL567815
Affinity INH = 47%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL567815
Affinity IC50 = 54uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL571227
Affinity INH = 104.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

Name CHEMBL572918
Affinity IC50 = 8uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL572918
Affinity INH > 100%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL572919
Affinity INH = 20%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL572920
Affinity INH = 9%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL573160
Affinity INH = 1%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL573174
Affinity INH = 70%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL573174
Affinity IC50 = 34uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL573429
Affinity INH = 63%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL573429
Affinity IC50 = 38uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL574200
Affinity IC50 = 2.7uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL574677
Affinity INH = 25%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL574677
Affinity IC50 = 104uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL574909
Affinity INH = 16%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575101
Affinity INH = 23%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575102
Affinity INH = 0%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575536
Affinity INH = 100%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575536
Affinity IC50 = 9.3uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575537
Affinity INH = 13%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575573
Affinity INH = 35%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575979
Affinity INH = 39%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL575979
Affinity IC50 = 63uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL576002
Affinity INH = 46%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL576002
Affinity IC50 = 58uM
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL576003
Affinity INH = 18%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL578040
Affinity INH = 23%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL583569
Affinity INH = 6%
Assay description Inhibition of Rac1 GTPase activity assessed as incorporation of BODIPY-GTP at 50 uM after 40 mins by nucleotide binding competition assay
-- Homologous single protein target assigned: RAC1_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19716293
Doc title Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.
PDB None

Name CHEMBL610247
Affinity INH = 99.4%
Assay description Inhibition of PDGF-BB-stimulated Rac1 activity in human aortic smooth muscle cells assessed as reduction of Rac1GTP level at 50 uM after 4 hrs by G-LISA relative to control
-- Direct single protein target assigned: RAC1_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19527032
Doc title Virtual screening approach for the identification of new Rac1 inhibitors.
PDB None

28 PDB entries for Rac1 and its protein partners


1FOE
Crystal structure of Rac1 in complex with the guanine nucleotide exchange region of Tiam1.

Entity type Code Description
polypeptide(L) Q60610 T-LYMPHOMA INVASION AND METASTASIS INDUCING PROTEIN 1
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE

1G4U
Modulation of host signaling by a bacterial mimic: structure of the Salmonella effector SptP bound to Rac1.

Entity type Code Description
polypeptide(L) P74873 PROTEIN TYROSINE PHOSPHATASE SPTP
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GDP GUANOSINE-5'-DIPHOSPHATE
Ligand AF3 ALUMINUM FLUORIDE

1I4D
The structural basis of Arfaptin-mediated cross-talk between Rac and Arf signalling pathways.

Entity type Code Description
polypeptide(L) P53365 ARFAPTIN 2
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GDP GUANOSINE-5'-DIPHOSPHATE

1I4L
The structural basis of Arfaptin-mediated cross-talk between Rac and Arf signalling pathways.

Entity type Code Description
polypeptide(L) P53365 ARFAPTIN 2
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GDP GUANOSINE-5'-DIPHOSPHATE

1I4T
The structural basis of Arfaptin-mediated cross-talk between Rac and Arf signalling pathways.

Entity type Code Description
polypeptide(L) P53365 ARFAPTIN 2
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

1MH1
The crystal structure of human rac1, a member of the rho-family complexed with a GTP analogue.

Entity type Code Description
polypeptide(L) P63000 RAC1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

1RYF
Alternative Splicing of Rac1 Generates Rac1b, a Self-activating GTPase

Entity type Code Description
polypeptide(L) P63000 ras-related C3 botulinum toxin substrate 1 isoform Rac1b
Ligand GDP GUANOSINE-5'-DIPHOSPHATE

1RYH
Alternative Splicing of Rac1 Generates Rac1b, a Self-activating GTPase

Entity type Code Description
polypeptide(L) P63000 ras-related C3 botulinum toxin substrate 1 isoform Rac1b
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

2FJU
Crystal structure of Rac1 bound to its effector phospholipase C-beta2.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
polypeptide(L) Q00722 1-phosphatidylinositol-4,5-bisphosphate phosphodiesterase beta 2
Ligand GSP 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE

2H7V
Yersinia virulence depends on mimicry of host rho-family nucleotide dissociation inhibitors.

Entity type Code Description
polypeptide(L) P63000 Migration-inducing protein 5
polypeptide(L) Q05608 Protein kinase ypkA
Ligand GDP GUANOSINE-5'-DIPHOSPHATE

2NZ8
The DH and PH Domains of Trio Coordinately Engage Rho GTPases for their Efficient Activation

Entity type Code Description
polypeptide(L) P63000 ras-related C3 botulinum toxin substrate 1 isoform Rac1
polypeptide(L) O75962 triple functional domain protein

2P2L
A Rac1-GDP trimer complex binds zinc with tetrahedral and octahedral coordination, displacing magnesium.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GDP GUANOSINE-5'-DIPHOSPHATE

2RMK
The Rac1 Polybasic Region Is Required for Interaction with Its Effector PRK1

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
polypeptide(L) Q16512 Serine/threonine-protein kinase N1
Ligand GCP PHOSPHOMETHYLPHOSPHONIC ACID GUANYLATE ESTER

2VRW
Crucial Structural Role for the Ph and C1 Domains of the Vav1 Exchange Factor.

Entity type Code Description
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) P27870 PROTO-ONCOGENE VAV

2WKP
A Genetically Encoded Photoactivatable Rac Controls the Motility of Living Cells.

Entity type Code Description
polypeptide(L) 2WKP NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) O49003 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) P63000 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GTP GUANOSINE-5'-TRIPHOSPHATE
Ligand FMN FLAVIN MONONUCLEOTIDE

2WKQ
A Genetically Encoded Photoactivatable Rac Controls the Motility of Living Cells.

Entity type Code Description
polypeptide(L) 2WKQ NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) O49003 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) P63000 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GTP GUANOSINE-5'-TRIPHOSPHATE
Ligand FMN FLAVIN MONONUCLEOTIDE

2WKR
A Genetically Encoded Photoactivatable Rac Controls the Motility of Living Cells.

Entity type Code Description
polypeptide(L) 2WKR NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) O49003 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
polypeptide(L) P63000 NPH1-1, RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1
Ligand GTP GUANOSINE-5'-TRIPHOSPHATE
Ligand FMN FLAVIN MONONUCLEOTIDE

2YIN
Multiple Factors Confer Specific Cdc42 and Rac Protein Activation by Dedicator of Cytokinesis (Dock) Nucleotide Exchange Factors.

Entity type Code Description
polypeptide(L) Q92608 DEDICATOR OF CYTOKINESIS PROTEIN 2
polypeptide(L) P63000 RAS-RELATED C3 BOTULINUM TOXIN SUBSTRATE 1

3B13
Structural basis for mutual relief of the Rac guanine nucleotide exchange factor DOCK2 and its partner ELMO1 from their autoinhibited forms.

Entity type Code Description
polypeptide(L) Q92608 Dedicator of cytokinesis protein 2
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1

3BJI
Structural basis of guanine nucleotide exchange mediated by the T-cell essential Vav1.

Entity type Code Description
polypeptide(L) P15498 Proto-oncogene vav
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1 precursor

3RYT
Plexins Are GTPase-Activating Proteins for Rap and Are Activated by Induced Dimerization.

Entity type Code Description
polypeptide(L) P70206 Plexin-A1
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

3SBD
Exome sequencing identifies recurrent somatic RAC1 mutations in melanoma.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

3SBE
Exome sequencing identifies recurrent somatic RAC1 mutations in melanoma.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

3SU8
A Dual Binding Mode for RhoGTPases in Plexin Signalling.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
polypeptide(L) O43157 Plexin-B1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

3SUA
A Dual Binding Mode for RhoGTPases in Plexin Signalling.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
polypeptide(L) O43157 Plexin-B1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

3TH5
Exome sequencing identifies recurrent somatic RAC1 mutations in melanoma.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

4GZL
RAC1P29S is a spontaneously activating cancer-associated GTPase.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GNP PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER

4GZM
RAC1P29S is a spontaneously activating cancer-associated GTPase.

Entity type Code Description
polypeptide(L) P63000 Ras-related C3 botulinum toxin substrate 1
Ligand GSP 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE