OSI-930 [Ligand Id: 9383] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1614710 (Osi 930, OSI-930, Osi-930)
  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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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  • colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
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  • fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of c-Raf B 7.39 pIC50 41 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
GtoPdb - - 7.39 pIC50 41 nM IC50 Cancer Res (2006) 66: 1015-24 [PMID:16424037]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of N-terminal GST-tagged recombinant kit (unknown origin) using poly(Glu:Tyr) as substrate by ELISA-based method B 7.1 pIC50 80 nM IC50 MedChemComm (2015) 6: 1518-1534
ChEMBL Inhibition of c-Kit B 7.54 pIC50 29 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6495-6499 [PMID:21920748]
GtoPdb The IC50 varied dependent on whether KIT was activated or unactivated, with the lower value measured for the activated enzyme. - 7.6 pIC50 25 nM IC50 Cancer Res (2006) 66: 1015-24 [PMID:16424037]
ChEMBL Inhibition of c-Kit B 8 pIC50 10 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
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 VEGFR2 B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
GtoPdb - - 8.05 pIC50 9 nM IC50 Cancer Res (2006) 66: 1015-24 [PMID:16424037]
ChEMBL Inhibition of KDR B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6495-6499 [PMID:21920748]
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 7.82 pIC50 15 nM IC50 Cancer Res (2006) 66: 1015-24 [PMID:16424037]
fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
GtoPdb - - 8.1 pIC50 8 nM IC50 Cancer Res (2006) 66: 1015-24 [PMID:16424037]

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]