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ChEMBL ligand: CHEMBL2316582 (D-824, D-824 DIMESYLATE, GZD-824, Gzd-824 dimesylate, GZD-824 DIMESYLATE, Hqp1351, HQP-1351, HQP1351, HQP-1351 DIMESYLATE, HQP1351 DIMESYLATE, Olverembatinib, Olverembatinib dimesylate) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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]