GNF-5 [Ligand Id: 8065] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1257423
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Mouse [ChEMBL: CHEMBL3099] [GtoPdb: 1923] [UniProtKB: P00520]
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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 (46 to 515 residues) expressed in bacterial expression system using EAIYAAPFAKKK as substrate measured every 20 secs in presence of [gamma-32P]ATP 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 5.7 pIC50 2000 nM IC50 ACS Med Chem Lett (2017) 8: 1042-1047 [PMID:29057048]
GtoPdb Inhibition of wild-type Abl in vitro. - 6.66 pIC50 220 nM IC50 Nature (2010) 463: 501-6 [PMID:20072125]
ChEMBL Inhibition of recombinant human c-ABL SH3/SH2/SH1 domain (46 to 515 residues) expressed in bacterial expression system using EAIYAAPFAKKK as substrate measured every 20 secs in presence of [gamma-32P]ATP B 7.77 pIC50 17 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]