ChEMBL ligand: CHEMBL247228 (GW770249X)
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] There should be some charts here, you may need to enable JavaScript!
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] There should be some charts here, you may need to enable JavaScript!
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] 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!
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] 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
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL	Inhibition of human CDK2	B	4.75	pIC50	17782.79	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Inhibition of human EGFR	B	5	pIC50	10000	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
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 cFMS	B	7.41	pIC50	38.9	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234]
ChEMBL	Inhibition of human PDGFR	B	7.56	pIC50	27.54	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
ChEMBL	Inhibition of fluorescent-labeled 3-(3-((3-(4-amino-5-(4-(3-(2-fluoro-5-(trifluoromethyl)phenyl)ureido)-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)amino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:2',1'-f]-[1,3,2]diazaborinin-4-ium-5-uide binding to human N-terminal GST/His-tagged RIPK1 (1 to 375 residues) expressed in baculovirus expression system by TR-FRET assay	B	8.69	pKi	2.04	nM	Ki	J Med Chem (2018) 61: 2384-2409 [PMID:29485864]
ChEMBL	Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay	B	6.6	pIC50	250	nM	IC50	ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635]
ChEMBL	Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido[1,2-a]indol-5-ium-2-sulfonate from human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by fluorescent ligand addition measured after 15 mins by fluorescence polarization assay	B	7.2	pIC50	63	nM	IC50	ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635]
ChEMBL	Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay	B	7.89	pIC50	13	nM	IC50	ACS Med Chem Lett (2013) 4: 1238-1243 [PMID:24900635]
ChEMBL	Inhibition of RIP1 (unknown origin) in ADP-glo assay	B	7.89	pIC50	13	nM	IC50	J Med Chem (2022) 65: 14971-14999 [PMID:36346971]
GtoPdb	IN an ADP-glo assay that measures the ADP produced during autophosphorylation of RIPK1 catalytic domain.	-	7.89	pIC50	13	nM	IC50	ACS Med Chem Lett (2013) 4: 1238-43 [PMID:24900635]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL	Inhibition of human Akt3	B	4.76	pIC50	17378.01	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
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 SRC	B	6.27	pIC50	537.03	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL	Inhibition of c-fms/Tie2 chimeric receptor transfected in 3T3 cell assessed as autophosphorylation activity	B	7.74	pIC50	18.3	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
ChEMBL	Inhibition of human Tie2 by HTRF method	B	7.87	pIC50	13.49	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL	Inhibition of human VEGFR1	B	8.07	pIC50	8.51	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
ChEMBL	Inhibition of human VEGFR2 by HTRF method	B	8.11	pIC50	7.76	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL	Inhibition of human VGFR3	B	8.12	pIC50	7.59	nM	IC50	Bioorg Med Chem Lett (2007) 17: 1773-1778 [PMID:17276055]

ChEMBL data shown on this page come from version 34:

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]