denfivontinib [Ligand Id: 8108] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4544478 (G-749, CPD 6, Denfivontinib, G749, DENFIVONTINIB) |
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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/Receptor-type tyrosine-protein kinase 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] |
| ChEMBL | Inhibition of FLT3 (unknown origin) using ULight-poly-GT peptide as substrate measured after 1 hr in presence of ATP by TR-FRET assay | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2025) 117: 130082-130082 [PMID:39708925] |
| GtoPdb | - | - | 9.4 | pIC50 | 0.4 | nM | IC50 | Blood (2014) 123: 2209-19 [PMID:24532805] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of AXL (unknown origin) preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by HTRF analysis | B | 8.03 | pIC50 | 9.38 | nM | IC50 | ACS Med Chem Lett (2025) 16: 410-419 [PMID:40110119] |
| 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 37:
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]
