velzatinib [Ligand Id: 11510] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5314917 (Idrx-42, M-4205)
  • 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 alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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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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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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
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 CSF1R (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 8.26 pIC50 5.5 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
GtoPdb Biochemical inhibitory potency - 8.26 pIC50 5.5 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
GtoPdb Biochemical inhibitory potency - 7.3 pIC50 50 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
ChEMBL Inhibition of PDGFRA (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 7.3 pIC50 50 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
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 PDGFRB (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 8.59 pIC50 2.6 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
GtoPdb Biochemical inhibitory potency - 8.59 pIC50 2.6 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
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 KIT (delta 560 to 576 residues) deletion/V654A double mutant autophosphorylation at Y703 in human GIST-430/654 harboring KIT (delta560 to 576 residues) deletion mutation and V654A point mutation incubated for 45 mins by Luminex-based bead assay B 7.32 pIC50 48 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
ChEMBL Inhibition of wild type KIT (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 7.36 pIC50 44 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
GtoPdb - - 7.36 pIC50 44 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
ChEMBL Inhibition of KIT (560 to 576 residues) deletion mutant autophosphorylation in human GIST430 cells harboring (560 to 576 residues) KIT deletion mutation incubated for 45 mins by Luminex-based bead assay B 8.4 pIC50 4 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
ChEMBL Inhibition of KIT N822K mutant autophosphorylation in human Kasumi 1 cells harboring KIT N822K mutation in exon 17 incubated for 45 mins by Luminex-based bead assay B 8.4 pIC50 4 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
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 (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 6.85 pIC50 141 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]
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 (unknown origin) using 33P-ATP as substrate incubated for 120 mins by radiometric kinase assay B 6.85 pIC50 141 nM IC50 J Med Chem (2023) 66: 2386-2395 [PMID:36728508]

ChEMBL data shown on this page come from version 35:

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]