Immunophilin FKBP1A

Peptidyl-prolyl cis-trans isomerase fkbp1a

Reviewed UniProt entries for Immunophilin FKBP1A and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
P18203 FKB1A_BOVIN Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (Calstabin-1) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) FKBP1A FKBP1 Bos taurus (Bovine) 108
P62942 FKB1A_HUMAN Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (Calstabin-1) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) FKBP1A FKBP1 FKBP12 Homo sapiens (Human) 108
P26883 FKB1A_MOUSE Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (Calstabin-1) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) Fkbp1a Fkbp1 Mus musculus (Mouse) 108
Q62658 FKB1A_RAT Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) Fkbp1a Fkbp1 Rattus norvegicus (Rat) 108
O42123 FKB1A_XENLA Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) fkbp1a Xenopus laevis (African clawed frog) 108
P62943 FKB1A_RABIT Peptidyl-prolyl cis-trans isomerase FKBP1A (PPIase FKBP1A) (EC 5.2.1.8) (12 kDa FK506-binding protein) (12 kDa FKBP) (FKBP-12) (Calstabin-1) (FK506-binding protein 1A) (FKBP-1A) (Immunophilin FKBP12) (Rotamase) FKBP1A FKBP1 FKBP12 Oryctolagus cuniculus (Rabbit) 108

Small molecules tested in Immunophilin FKBP1A binding assays:

888 datapoints for 699 distinct small molecules


Name CHEMBL10
Affinity Residual Activity = 96%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL10
Affinity Residual Activity = 86%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL101683
Affinity Residual Activity = 88%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL101683
Affinity Residual Activity = 69%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL102346
Affinity Residual Activity = 98%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL102346
Affinity Residual Activity = 99%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104264
Affinity Residual Activity = 62%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104264
Affinity Residual Activity = 120%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104279
Affinity Residual Activity = 104%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104279
Affinity Residual Activity = 102%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104468
Affinity Residual Activity = 107%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL104468
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL107101
Affinity IC50 = 8.2nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB None

Name CHEMBL107603
Affinity Ki > 10000nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL1076555
Affinity Residual Activity = 106%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1076555
Affinity Residual Activity = 103%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL107698
Affinity Ki = 170nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL107774
Affinity IC50 = 64nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB None

Name CHEMBL108247
Affinity Ki = 130nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL108296
Affinity IC50 = 15nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB None

Name CHEMBL108383
Affinity IC50 = 40nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB None

Name CHEMBL108383
Affinity IC50 = 40nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB None

Name CHEMBL109278
Affinity IC50 = 0.2uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL109278
Affinity Ki = 0.23uM
Assay description Inhibition of FKBP12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL110674
Affinity IC50 = 8.2nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB 1BL4 - (AP1)

Name CHEMBL110674
Affinity IC50 = 8.2nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB 1BL4 - (AP1)

Name CHEMBL110674
Affinity IC50 = 1.8nM
Assay description Inhibition of binding to Phe36Val (F36V) mutant of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12951089
Doc title Regulation of gene expression by synthetic dimerizers with novel specificity.
PDB 1BL4 - (AP1)

Name CHEMBL111364
Affinity Residual Activity = 91%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL111364
Affinity Residual Activity = 84%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1182777
Affinity Residual Activity = 39%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1182777
Affinity Residual Activity = 98%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL118291
Affinity Ki = 3400nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL1186409
Affinity Residual Activity = 84%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1186409
Affinity Residual Activity = 79%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL118662
Affinity Ki = 3800nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL118716
Affinity Ki = 10000nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL118858
Affinity Ki = 8.7nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL118884
Affinity Ki = 7nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL118937
Affinity Ki = 6nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL118978
Affinity Ki = 420nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL119155
Affinity Ki = 130nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL119228
Affinity Ki = 11nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL119280
Affinity Ki = 12.2nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL119377
Affinity Ki = 10000nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL119571
Affinity Ki = 8.9nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL119580
Affinity Ki = 86nM
Assay description Inhibitory activity against FK506 binding protein 12
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139466
Doc title Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
PDB None

Name CHEMBL120077
Affinity Residual Activity = 107%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL120077
Affinity Residual Activity = 114%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL120138
Affinity IC50 = 22.3uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL120252
Affinity IC50 > 200uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL120303
Affinity Ki = 210nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL120311
Affinity Ki = 790nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL120385
Affinity IC50 = 124.1uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL120492
Affinity IC50 = 116.7uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL120518
Affinity Ki = 30nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL120550
Affinity Ki = 240nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL120630
Affinity Ki = 310nM
Assay description In vitro inhibition of rotamase activity of FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_RAT (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12139467
Doc title Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
PDB None

Name CHEMBL120675
Affinity IC50 = 21.6uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL1213336
Affinity Active
Assay description Binding affinity to human FKBP12 in Jurkat cells at 11 uM after 24 hrs using anti-human FKBP12 antibody
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19330012
Doc title Ligand-directed tosyl chemistry for protein labeling in vivo.
PDB None

Name CHEMBL1221601
Affinity Residual Activity = 78%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1221601
Affinity Residual Activity = 88%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1231533
Affinity Residual Activity = 104%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1231533
Affinity Residual Activity = 106%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL123292
Affinity Ki = 3.4uM
Assay description Inhibition constant(Ki) for inhibition of PPIase activity of human FK506 binding protein 12 (Conc=14 nM) of FKBPs family
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL123292
Affinity IC50 = 3.6uM
Assay description Compound was evaluated for its inhibitory effect on human FK506 binding protein 12 by means of protease-coupled PPIase assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10479292
Doc title Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties.
PDB None

Name CHEMBL1240885
Affinity Residual Activity = 95%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1240885
Affinity Residual Activity = 91%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL126031
Affinity Ki = 52nM
Assay description The compound was tested for binding affinity against rotamase
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9767630
Doc title Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
PDB None

Name CHEMBL126568
Affinity Ki = 10nM
Assay description The compound was tested for binding affinity against rotamase
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9767630
Doc title Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
PDB 1FKG - (SB3)

Name CHEMBL126568
Affinity Ki = 0.01uM
Assay description Inhibition of FKBP12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB 1FKG - (SB3)

Name CHEMBL126568
Affinity Ki = 17nM
Assay description The compound was tested for binding affinity against rotamase
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9767630
Doc title Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
PDB 1FKG - (SB3)

Name CHEMBL1272245
Affinity Not Active
Assay description Inhibition of FKBP12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20932746
Doc title Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.
PDB None

Name CHEMBL1289494
Affinity Residual Activity = 95%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1289494
Affinity Residual Activity = 85%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL129537
Affinity Ki = 165nM
Assay description The compound was tested for binding affinity against rotamase
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9767630
Doc title Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
PDB None

Name CHEMBL129537
Affinity Ki = 130nM
Assay description The compound was tested for binding affinity against rotamase
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9767630
Doc title Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
PDB None

Name CHEMBL129537
Affinity IC50 = 2.11uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL13045
Affinity Residual Activity = 98%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL13045
Affinity Residual Activity = 89%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1317546
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1317546
Affinity Residual Activity = 104%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1331734
Affinity Residual Activity = 76%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1331734
Affinity Residual Activity = 119%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL13485
Affinity Residual Activity = 102%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL13485
Affinity Residual Activity = 115%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1363184
Affinity Residual Activity = 90%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1363184
Affinity Residual Activity = 76%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1398474
Affinity Residual Activity = 70%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1398474
Affinity Residual Activity = 98%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL139966
Affinity IC50 = 529nM
Assay description The compound was tested for binding affinity against human FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10543889
Doc title Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.
PDB None

Name CHEMBL140442
Affinity IC50 = 3.4nM
Assay description Compound was tested in vitro for its ability to compete with immobilized FK506 for binding to biotinylated FK506 binding protein 12 in a competitive binding assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10091702
Doc title Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity.
PDB None

Name CHEMBL146203
Affinity Ki = 103nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL146204
Affinity Ki = 210nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL146527
Affinity Ki = 470nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL146804
Affinity Ki = 760nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL146919
Affinity Ki = 15nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL14756
Affinity IC50 = 19nM
Assay description Binding affinity for Mutant F36V-FK506 binding protein by competitive assay based on fluorescence polarization.
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10737745
Doc title Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.
PDB None

Name CHEMBL147712
Affinity Ki = 170nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148435
Affinity Ki = 17nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB 1FKG - (SB3)

Name CHEMBL148446
Affinity Ki = 17nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148494
Affinity Ki = 34nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148502
Affinity Ki = 20000nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148516
Affinity Ki = 95nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148517
Affinity Ki = 9nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148555
Affinity Ki = 742nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL148621
Affinity Ki = 131nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL14885
Affinity IC50 = 40nM
Assay description Binding affinity for Mutant F36V-FK506 binding protein by competitive assay based on fluorescence polarization.
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10737745
Doc title Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.
PDB None

Name CHEMBL148982
Affinity Ki = 40nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL149011
Affinity Ki = 332nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL14903
Affinity IC50 = 94nM
Assay description Binding affinity for Mutant F36V-FK506 binding protein by competitive assay based on fluorescence polarization.
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10737745
Doc title Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.
PDB None

Name CHEMBL149155
Affinity Ki = 35000nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL149192
Affinity Ki = 7.5nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB 1F40 - (GPI)

Name CHEMBL149314
Affinity Ki = 42nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL149373
Affinity Ki = 82nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL1496098
Affinity Residual Activity = 117%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1496098
Affinity Residual Activity = 89%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL149669
Affinity Ki = 116nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL149707
Affinity Ki = 32nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL149708
Affinity Ki = 8000nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL150062
Affinity Ki = 18nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL150100
Affinity Ki = 13nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL150120
Affinity Ki = 3nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL150229
Affinity Ki = 72nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151326
Affinity Ki = 6000nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151327
Affinity Ki = 78nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151517
Affinity Ki = 194nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151727
Affinity Ki = 0.5nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151841
Affinity Ki = 1nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB None

Name CHEMBL151857
Affinity IC50 = 1.65uM
Assay description Concentration required to produce a half-maximal FP signalat against FK506 binding protein 12 at ligand concentration of 100 nM
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL151857
Affinity Ki = 1300nM
Assay description Binding affinity of compound for FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL152022
Affinity Ki = 482nM
Assay description Binding affinity of compound for FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL152022
Affinity IC50 = 0.98uM
Assay description Concentration required to produce a half-maximal FP signalat against FK506 binding protein 12 at ligand concentration of 100 nM
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL155333
Affinity Residual Activity = 97%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL155333
Affinity Residual Activity = 101%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL155511
Affinity Ki = 32nM
Assay description Binding affinity of compound for FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL155511
Affinity IC50 = 0.25uM
Assay description Concentration required to produce a half-maximal FP signalat against FK506 binding protein 12 at ligand concentration of 100 nM
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL155512
Affinity Ki = 526nM
Assay description Binding affinity of compound for FK506 binding protein 12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL155512
Affinity IC50 = 0.41uM
Assay description Concentration required to produce a half-maximal FP signalat against FK506 binding protein 12 at ligand concentration of 100 nM
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/10741553
Doc title Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
PDB None

Name CHEMBL1650802
Affinity IC50 > 30uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650803
Affinity IC50 = 2.6uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650804
Affinity IC50 = 3.1uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650805
Affinity IC50 = 2.8uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650943
Affinity IC50 = 0.26uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650944
Affinity IC50 > 30uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650945
Affinity IC50 = 4.2uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650946
Affinity IC50 = 0.2uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650947
Affinity IC50 = 0.12uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650948
Affinity IC50 = 0.15uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650949
Affinity IC50 = 0.07uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL1650950
Affinity IC50 = 0.32uM
Assay description Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21142106
Doc title Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
PDB None

Name CHEMBL17331
Affinity Residual Activity = 126%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL17331
Affinity Residual Activity = 71%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL174426
Affinity Residual Activity = 97%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL174426
Affinity Residual Activity = 104%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL178537
Affinity Ki app = 250nM
Assay description Compound was tested for inhibitory activity against FK506 binding protein 12 (FKBP12)
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/7241506
Doc title New analgesic drugs derived from phencyclidine.
PDB None

Name CHEMBL179583
Affinity Residual Activity = 113%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL179583
Affinity Residual Activity = 110%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802485
Affinity Residual Activity = 66%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802485
Affinity Residual Activity = 117%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802727
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802727
Affinity Residual Activity = 110%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802728
Affinity Residual Activity = 113%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL1802728
Affinity Residual Activity = 55%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL188762
Affinity Residual Activity = 101%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL188762
Affinity Residual Activity = 123%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL191003
Affinity Residual Activity = 98%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL191003
Affinity Residual Activity = 83%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL191384
Affinity Residual Activity = 53%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL191384
Affinity Residual Activity = 102%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL200381
Affinity Residual Activity = 107%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL200381
Affinity Residual Activity = 96%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL200999
Affinity Ki = 183nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201201
Affinity Ki = 126nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201214
Affinity Ki = 82nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201265
Affinity Ki = 266nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201359
Affinity Ki = 156nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201714
Affinity Ki = 88nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201785
Affinity Ki = 236nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201849
Affinity Ki = 72nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201850
Affinity Ki = 100nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201963
Affinity Ki = 360nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL201970
Affinity Ki = 60nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202000
Affinity Ki = 330nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202009
Affinity Ki = 123nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202012
Affinity Ki = 69nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202048
Affinity Ki = 34nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202066
Affinity Ki = 583nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202088
Affinity Ki = 110nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202097
Affinity Ki = 225nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202101
Affinity Ki = 201nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202102
Affinity Ki = 46nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202108
Affinity Ki = 244nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202123
Affinity Ki = 150nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202171
Affinity Ki = 591nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202180
Affinity Ki = 143nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202217
Affinity Ki = 20800nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202227
Affinity Ki = 71nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202357
Affinity Ki = 1000nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202382
Affinity Ki = 171nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202446
Affinity Ki = 3100nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202465
Affinity Ki = 152nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202517
Affinity Ki = 238nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202592
Affinity Ki = 590nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL202655
Affinity Ki = 107nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL203094
Affinity Ki = 279nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL203250
Affinity Ki = 131nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL203358
Affinity Ki = 84nM
Assay description Inhibition of FKBP12 rotamase activity
-- Direct single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16451085
Doc title Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
PDB None

Name CHEMBL203644
Affinity Residual Activity = 92%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL203644
Affinity Residual Activity = 113%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2052020
Affinity Ki = 0.7nM
Assay description Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity
-- Homologous single protein target assigned: FKB1A_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/9857082
Doc title Immunophilins: beyond immunosuppression.
PDB 1FKD - (818)

Name CHEMBL2057219
Affinity IC50 = 4.5uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2057227
Affinity IC50 = 0.06uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058222
Affinity IC50 = 1.8uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058223
Affinity IC50 = 1.2uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058224
Affinity IC50 = 1.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058225
Affinity IC50 = 10.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058226
Affinity IC50 = 4.6uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058227
Affinity IC50 = 3.8uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058228
Affinity IC50 = 1.9uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058229
Affinity IC50 = 1.9uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058230
Affinity IC50 = 8.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058231
Affinity IC50 = 9.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058232
Affinity IC50 = 1.09uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058233
Affinity IC50 = 0.32uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058234
Affinity IC50 = 0.8uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058235
Affinity IC50 = 6.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058236
Affinity IC50 = 7.6uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058237
Affinity IC50 = 0.6uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058238
Affinity IC50 = 1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058239
Affinity IC50 = 5.1uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058240
Affinity IC50 = 2.4uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058494
Affinity IC50 = 0.67uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058495
Affinity IC50 = 0.23uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058496
Affinity IC50 = 1.18uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058497
Affinity Not Active
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058498
Affinity IC50 = 1.5uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058499
Affinity IC50 = 2.57uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058500
Affinity IC50 = 1.2uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058787
Affinity IC50 = 0.021uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058788
Affinity IC50 = 0.66uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058789
Affinity IC50 = 0.75uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058790
Affinity IC50 > 100uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058791
Affinity IC50 = 0.2uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058792
Affinity IC50 > 50uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058793
Affinity IC50 > 50uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058794
Affinity IC50 = 0.115uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058795
Affinity IC50 > 50uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058796
Affinity IC50 = 0.003uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058797
Affinity IC50 = 0.45uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058798
Affinity IC50 > 100uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058799
Affinity IC50 = 1.4uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058800
Affinity IC50 = 0.87uM
Assay description Binding affinity to FKBP12 by competitive fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455398
Doc title Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058801
Affinity IC50 = 0.8uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058802
Affinity IC50 = 0.55uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058803
Affinity IC50 = 1.29uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058804
Affinity IC50 = 3.38uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2058805
Affinity IC50 = 17.1uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059023
Affinity IC50 = 2.45uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059024
Affinity IC50 = 0.1uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059025
Affinity IC50 = 1.05uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059026
Affinity IC50 = 0.1uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059027
Affinity IC50 = 0.15uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059028
Affinity IC50 > 100uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059029
Affinity IC50 = 0.06uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059029
Affinity IC50 = 0.06uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059030
Affinity IC50 = 2.2uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059031
Affinity IC50 = 0.31uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059032
Affinity IC50 = 2.78uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059033
Affinity IC50 = 0.13uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059033
Affinity IC50 = 0.32uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059034
Affinity IC50 = 0.343uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059035
Affinity IC50 = 0.47uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059036
Affinity IC50 = 0.51uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059237
Affinity IC50 = 0.05uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059237
Affinity IC50 = 0.06uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059238
Affinity IC50 = 0.05uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059239
Affinity IC50 = 0.06uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL2059240
Affinity IC50 = 0.57uM
Assay description Binding affinity to FKBP12 by fluorescence polarization assay
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22455444
Doc title Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
PDB None

Name CHEMBL210618
Affinity Residual Activity = 80%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL210618
Affinity Residual Activity = 124%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL210833
Affinity Residual Activity = 88%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL210833
Affinity Residual Activity = 95%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL21156
Affinity Residual Activity = 100%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL21156
Affinity Residual Activity = 80%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2205015
Affinity Ki = 19nM
Assay description Inhibition of FKBP12
-- Homologous single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21413808
Doc title Synopsis of some recent tactical application of bioisosteres in drug design.
PDB 1J4R - (001)

Name CHEMBL221271
Affinity Residual Activity = 125%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL221271
Affinity Residual Activity = 88%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218925
Affinity Residual Activity = 110%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218925
Affinity Residual Activity = 103%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218926
Affinity Residual Activity = 89%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218926
Affinity Residual Activity = 102%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218927
Affinity Residual Activity = 80%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218927
Affinity Residual Activity = 84%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218928
Affinity Residual Activity = -17%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB 1FKB - (RAP)

Name CHEMBL2218928
Affinity Residual Activity = 4%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB 1FKB - (RAP)

Name CHEMBL2218929
Affinity Residual Activity = 76%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218929
Affinity Residual Activity = 105%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218930
Affinity Residual Activity = 111%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218930
Affinity Residual Activity = 75%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218931
Affinity Residual Activity = 94%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218931
Affinity Residual Activity = 110%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218932
Affinity Residual Activity = 75%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218932
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218933
Affinity Residual Activity = 77%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218933
Affinity Residual Activity = 89%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218934
Affinity Residual Activity = 36%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218934
Affinity Residual Activity = 90%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218935
Affinity Residual Activity = 93%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218935
Affinity Residual Activity = 105%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218936
Affinity Residual Activity = 96%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218936
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218937
Affinity Residual Activity = 100%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218937
Affinity Residual Activity = 112%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218938
Affinity Residual Activity = 76%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218938
Affinity Residual Activity = 102%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218939
Affinity Residual Activity = 95%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218939
Affinity Residual Activity = 74%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218940
Affinity Residual Activity = 118%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218940
Affinity Residual Activity = 79%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218941
Affinity Residual Activity = 84%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL2218941
Affinity Residual Activity = 105%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL222102
Affinity Residual Activity = 89%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL222102
Affinity Residual Activity = 60%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL226838
Affinity Residual Activity = 110%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL226838
Affinity Residual Activity = 121%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL233001
Affinity Residual Activity = 113%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL233001
Affinity Residual Activity = 122%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL23327
Affinity Residual Activity = 101%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL23327
Affinity Residual Activity = 109%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL235036
Affinity Kd = 231uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235037
Affinity Kd = 100uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235038
Affinity Kd = 357uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235039
Affinity Kd = 576uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235078
Affinity Kd > 1400uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235080
Affinity Kd > 5000uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235103
Affinity Kd = 426uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235104
Affinity Kd = 5.6uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235114
Affinity Kd = 1285uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235260
Affinity Kd > 4000uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235297
Affinity Kd > 1500uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235298
Affinity Kd > 2500uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235467
Affinity Kd = 755uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235468
Affinity Kd = 231uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235469
Affinity Kd > 1500uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235477
Affinity Kd = 552uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235641
Affinity Residual Activity = 99%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL235641
Affinity Residual Activity = 95%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL235658
Affinity Residual Activity = 82%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL235658
Affinity Residual Activity = 105%
Assay description Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12
-- Direct protein complex subunits assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23398362
Doc title A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
PDB None

Name CHEMBL235681
Affinity Kd = 123uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235683
Affinity Kd = 167uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235713
Affinity Kd > 1000uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235898
Affinity Kd > 3000uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235914
Affinity Kd = 289uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235926
Affinity Kd > 1500uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235927
Affinity Kd > 1000uM
Assay description Binding affinity to human FKBP12 expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: FKB1A_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18038971
Doc title Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors.
PDB None

Name CHEMBL235928
Affinity Kd = 576uM