compound 27 [PMID: 24900635] [Ligand Id: 10133] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL247228 (GW770249X)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
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  • receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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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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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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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: 18041803] [UniProtKB: P09619P16234]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]