denfivontinib [Ligand Id: 8108] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4544478 (Denfivontinib, G-749)
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3-D835Y mutant (unknown origin) B 9.22 pIC50 0.6 nM IC50 J Med Chem (2020) 63: 12403-12428 [PMID:32659083]
ChEMBL Inhibition of FLT3 (unknown origin) by ADP-Glo kinase assay B 9.4 pIC50 0.4 nM IC50 J Med Chem (2020) 63: 12403-12428 [PMID:32659083]
GtoPdb - - 9.4 pIC50 0.4 nM IC50 Blood (2014) 123: 2209-19 [PMID:24532805]
MER proto-oncogene, tyrosine kinase in Human [GtoPdb: 1837] [UniProtKB: Q12866]
GtoPdb - - 9 pIC50 1 nM IC50 Blood (2014) 123: 2209-19 [PMID:24532805]

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]