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 ABL1 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 | TBD: TBD | B | 6.03 | pIC50 | 935 | nM | IC50 | US-11649218-B2. C-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same (2023) |
| ChEMBL | Inhibition of Abl (unknown origin) | B | 6.56 | pIC50 | 273 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| 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 ABL1 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 36:
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]
