Bcr-abl inhibitor GNF-2 [Ligand Id: 5935] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL483847 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Inhibition of recombinant human c-ABL SH1 domain expressed in sf9 insect cells after 30 mins in presence of [gamma-32P]ATP by autoradiography | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8120-8135 [PMID:30137981] |
| ChEMBL | Inhibition of recombinant human His-tagged full length ABL1 allosteric site expressed in baculovirus expression system by TR-FRET assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1042-1047 [PMID:29057048] |
| ChEMBL | Inhibition of recombinant human c-ABL SH3/SH2/SH1 domain (46 to 531 residues) expressed in sf9 insect cells after 30 mins in presence of [gamma-32P]ATP by autoradiography | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2018) 61: 8120-8135 [PMID:30137981] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3099] [GtoPdb: 1923] [UniProtKB: P00520] | ||||||||
| ChEMBL | Inhibition of Bcr-Abl T315I mutant in mouse BA/F3 cells assessed as cell growth inhibition | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2010) 53: 6934-6946 [PMID:20828158] |
| ChEMBL | Inhibition of Bcr-Abl E505K mutant in mouse BA/F3 cells assessed as cell growth inhibition | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2010) 53: 6934-6946 [PMID:20828158] |
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]
