olverembatinib [Ligand Id: 10630] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2316582 (D-824, D-824 DIMESYLATE, GZD-824, GZD-824 DIMESYLATE, Hqp1351, HQP-1351, HQP1351, HQP-1351 DIMESYLATE, HQP1351 DIMESYLATE, Olverembatinib, Olverembatinib dimesylate)
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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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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  • 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
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of His tagged recombinant human FGFR1 (308 to 731 residues) expressed in baculovirus expression system incubated for 1.5 hrs in the presence of ATP by Z'-LYTE kinase assay B 8.38 pIC50 4.14 nM IC50 Eur J Med Chem (2021) 214: 113205-113205 [PMID:33556787]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.68 pIC50 2078 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of PDGFRalpha (unknown origin) incubated for 1.5 hrs in the presence of ATP by Z'-LYTE kinase assay B 8.68 pIC50 2.08 nM IC50 Eur J Med Chem (2021) 214: 113205-113205 [PMID:33556787]
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 Binding affinity to phosphorylated ABL1 T315I mutant (unknown origin) after 1 hr B 8.49 pKd 3.2 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to non phosphorylated ABL1 F317I mutant (unknown origin) after 1 hr B 8.74 pKd 1.8 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to non phosphorylated ABL1 T315I mutant (unknown origin) after 1 hr B 9.15 pKd 0.71 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to non phosphorylated ABL1 Q252H mutant (unknown origin) after 1 hr B 9.34 pKd 0.46 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to phosphorylated wild type ABL1 (unknown origin) after 1 hr B 9.47 pKd 0.34 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
GtoPdb Binding affinity for nonphosphorylated Abl1 as determined using an active-site-dependent competitive binding assay (KINOMEscan). - 9.49 pKd 0.32 nM Kd J Med Chem (2013) 56: 879-94 [PMID:23301703]
ChEMBL Binding affinity to non phosphorylated wild type ABL1 (unknown origin) after 1 hr B 9.49 pKd 0.32 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to phosphorylated ABL1 E255K mutant (unknown origin) after 1 hr B 9.55 pKd 0.28 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to phosphorylated ABL1 M351T mutant (unknown origin) after 1 hr B 9.64 pKd 0.23 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Binding affinity to non phosphorylated ABL1 H396P mutant (unknown origin) after 1 hr B 9.74 pKd 0.18 nM Kd J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay B 9.15 pIC50 0.71 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay B 9.17 pIC50 0.68 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay B 9.46 pIC50 0.35 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay B 9.46 pIC50 0.35 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay B 9.47 pIC50 0.34 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
GtoPdb Inhibition of wild type Abl1 kinase activity was determined using the proprietary FRET-based Z′-Lyte assay. - 9.47 pIC50 0.34 nM IC50 J Med Chem (2013) 56: 879-94 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay B 9.54 pIC50 0.29 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay B 9.57 pIC50 0.27 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
ChEMBL Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay B 9.82 pIC50 0.15 nM IC50 J Med Chem (2013) 56: 879-894 [PMID:23301703]
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 His tagged recombinant human FLT3 (564 to 958 residues) expressed in baculovirus expression system incubated for 1.5 hrs in the presence of ATP by Z'-LYTE kinase assay B 8.88 pIC50 1.33 nM IC50 Eur J Med Chem (2021) 214: 113205-113205 [PMID:33556787]

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]