ChEMBL ligand: CHEMBL2010872 (BOL-303213X, Cep 11981, Cep-11981, CEP-11981, CEP11981)
A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] There should be some charts here, you may need to enable JavaScript!
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] There should be some charts here, you may need to enable JavaScript!
aurora kinase A/Aurora kinase A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] There should be some charts here, you may need to enable JavaScript!
M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] There should be some charts here, you may need to enable JavaScript!
Testicular receptor 4/Nuclear receptor subfamily 2 group C member 2 in Human [ChEMBL: CHEMBL5716] [GtoPdb: 614] [UniProtKB: P49116] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] There should be some charts here, you may need to enable JavaScript!
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 7 in Human [GtoPdb: 2082] [UniProtKB: O43318] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
A2A receptor/Adenosine receptor A2a 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]
TEK receptor tyrosine kinase/Angiopoietin-1 receptor 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]
aurora kinase A/Aurora kinase 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]
neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor 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]
casein kinase 1 alpha 1/Casein kinase I isoform 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]
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor 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]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 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]
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]
ret proto-oncogene/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/Proto-oncogene 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]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase 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]
serine/threonine kinase 3/Serine/threonine-protein kinase 3 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]
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]
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 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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]
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 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]