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
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
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
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

Small molecules tested in Immunophilin FKBP1A binding assays:

893 datapoints for 700 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 = 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 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 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 = 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 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 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 = 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 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 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 = 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 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 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 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 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 = 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 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 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 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 = 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 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 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 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 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 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 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 CHEMBL126077
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 CHEMBL126077
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 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 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 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 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 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 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 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 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 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 CHEMBL151857
Affinity IC50 = 1.65uM
Assay description Concentration required to produce a half-maximal FP signal at 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 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 signal at 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 IC50 = 0.25uM
Assay description Concentration required to produce a half-maximal FP signal at 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 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 CHEMBL155512
Affinity IC50 = 0.41uM
Assay description Concentration required to produce a half-maximal FP signal at 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 CHEMBL162
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 CHEMBL162
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 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 CHEMBL1725279
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 CHEMBL1725279
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 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 = 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 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 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 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 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 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 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 = 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 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 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 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 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 = 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 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 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 = 0.32uM
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 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 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 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 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 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 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 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 = 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 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 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 = 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 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 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 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 CHEMBL2218937
Affinity Residual Activity = 109%
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 = 117%
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 = 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 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 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 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 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 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 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 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 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 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 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 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 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 CHEMBL2348604
Affinity Ki = 0.5uM
Assay description Binding affinity to FKBP12 (unknown origin) by competitive fluorescence polarization assay
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23647266
Doc title Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
PDB None

Name CHEMBL2348605
Affinity Ki = 2.8uM
Assay description Binding affinity to FKBP12 (unknown origin) by competitive fluorescence polarization assay
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23647266
Doc title Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
PDB None

Name CHEMBL2348606
Affinity Ki = 27.7uM
Assay description Binding affinity to FKBP12 (unknown origin) by competitive fluorescence polarization assay
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23647266
Doc title Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
PDB None

Name CHEMBL2348607
Affinity Ki = 0.87uM
Assay description Binding affinity to FKBP12 (unknown origin) by competitive fluorescence polarization assay
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23647266
Doc title Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
PDB None

Name CHEMBL2348608
Affinity Ki = 2.1uM
Assay description Binding affinity to FKBP12 (unknown origin) by competitive fluorescence polarization assay
-- Direct single protein target assigned: FKB1A_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23647266
Doc title Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control.
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 = 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 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 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 col