Flt-3 inhibitor II [Ligand Id: 5971] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL377193
  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 18041803] [UniProtKB: P09619P16234]
  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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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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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 18041803] [UniProtKB: P09619P16234]
GtoPdb - - 6.77 pIC50 171 nM IC50 J Med Chem (2006) 49: 3101-15 [PMID:16722630]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
ChEMBL Inhibition of endogenous PDGFR in Swiss3T3 fibroblasts B 6.52 pIC50 300 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of human PDGFR beta B 6.77 pIC50 171 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
GtoPdb - - 6.77 pIC50 171 nM IC50 J Med Chem (2006) 49: 3101-15 [PMID:16722630]
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 DNA synthesis in IL3 dependent FDC-P1 cells expressing wild-type KIT F 6.3 pIC50 500 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
ChEMBL Inhibition of DNA synthesis in IL3 dependent FDC-P1 cells expressing KIT V558D mutant F 6.3 pIC50 500 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of recombinant Abl B 5.89 pIC50 1300 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Antiproliferative activity against mouse 32Dcl3 cell line expressing FLT3-ITD F 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
ChEMBL Antiproliferative activity against mouse 32Dcl3 cell line expressing wild-type FLT3 F 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
ChEMBL Inhibition of endogenous FLT3 in EOL1 cells B 7.4 pIC50 40 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]
GtoPdb - - 7.48 pIC50 33 nM IC50 J Med Chem (2006) 49: 3101-15 [PMID:16722630]
ChEMBL Inhibition of human FLT3 B 7.48 pIC50 33 nM IC50 J Med Chem (2006) 49: 3101-3115 [PMID:16722630]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]