CEP-11981 [Ligand Id: 8189] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2010872 (CEP-11981, BOL-303213X)
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
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  • Testicular receptor 4/Nuclear receptor subfamily 2 group C member 2 in Human [ChEMBL: CHEMBL5716] [GtoPdb: 614] [UniProtKB: P49116]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
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  • serine/threonine kinase 3/Serine/threonine-protein kinase MST2 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
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  • BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
  • BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Mouse [ChEMBL: CHEMBL3343] [GtoPdb: 1940] [UniProtKB: P16277]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • mitogen-activated protein kinase kinase kinase 7 in Human [GtoPdb: 2082] [UniProtKB: O43318]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Inhibition of adenosine A2A receptor B 6.3 pKi 500 nM Ki J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of human ALK using ATP as substrate B 6.88 pIC50 132 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CK1 using ATP as substrate B 7.32 pIC50 48 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of human FGFR1 using ATP as substrate B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
GtoPdb - - 7.89 pIC50 13 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Inhibition of human FGFR3 using ATP as substrate B 7.05 pIC50 89 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human Erg expressed CHO cells B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Inhibition of human FMS using ATP as substrate B 7.11 pIC50 78 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Inhibition of muscarinic M4 receptor B 5.54 pKi 2900 nM Ki J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
GtoPdb - - 8.52 pIC50 3 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
ChEMBL Inhibition of human TRK-A using ATP as substrate B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
GtoPdb - - 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
ChEMBL Inhibition of human TRK-B using ATP as substrate B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
Testicular receptor 4/Nuclear receptor subfamily 2 group C member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5716] [GtoPdb: 614] [UniProtKB: P49116]
ChEMBL Inhibition of human TAK1 using ATP as substrate B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of human PDGFRalpha using ATP as substrate B 6.61 pIC50 246 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of human Aurora-A using ATP as substrate B 7.38 pIC50 42 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
ChEMBL Inhibition of human CHK2 using ATP as substrate B 6.85 pIC50 140 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
serine/threonine kinase 3/Serine/threonine-protein kinase MST2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
ChEMBL Inhibition of human MST2 using ATP as substrate B 7.68 pIC50 21 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
GtoPdb - - 7.68 pIC50 21 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
GtoPdb - - 8.1 pIC50 8 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3343] [GtoPdb: 1940] [UniProtKB: P16277]
ChEMBL Inhibition of mouse BLK using ATP as substrate B 8.1 pIC50 8 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of human BTK using ATP as substrate B 7.03 pIC50 93 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human FLT3 using ATP as substrate B 7.15 pIC50 71 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
GtoPdb - - 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
ChEMBL Inhibition of human RET using ATP as substrate B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of human cSrc using ATP as substrate B 7.43 pIC50 37 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of human Tie2 expressed in porcine PAE145 cells cotransfected with chimeric rat TRK-A/KDR receptor after 1 hr by immunofluorescence assay B 7.3 pIC50 50 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
GtoPdb - - 7.59 pIC50 26 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
ChEMBL Inhibition of human recombinant Tie2 expressed in baculovirus expression system using GST-PLCgamma as substrate after 1 hr by time-resolved fluorescence analysis B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
GtoPdb - - 8.52 pIC50 3 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
ChEMBL Inhibition of human VEGFR1 using ATP as substrate B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of human VEGFR2 expressed in porcine PAE145 cells cotransfected with chimeric rat TRK-A/KDR receptor after 1 hr by immunofluorescence assay B 8 pIC50 <10 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
ChEMBL Inhibition of human recombinant VEGF-R2 expressed in baculovirus expression system using GST-PLCgamma as substrate after 1 hr by time-resolved fluorescence analysis B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2012) 55: 903-913 [PMID:22148921]
GtoPdb - - 8.4 pIC50 4 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]
mitogen-activated protein kinase kinase kinase 7 in Human [GtoPdb: 2082] [UniProtKB: O43318]
GtoPdb - - 7.85 pIC50 14 nM IC50 J. Med. Chem. (2012) 55: 903-13 [PMID:22148921]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]