BO1 [Ligand Id: 8963] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL255738
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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 Mixed-type inhibition of histidine-tagged human recombinant ABL expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using abtide peptide as substrate B 6.33 pKi 470 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of histidine-tagged human recombinant ABL T315I mutant expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using abtide peptide as substrate B 6.35 pKi 450 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of histidine-tagged human recombinant ABL T315I mutant expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using ATP as substrate B 6.4 pKi 400 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of histidine-tagged human recombinant ABL expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using abtide peptide as substrate B 6.92 pKi 120 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of histidine-tagged human recombinant ABL expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using ATP as substrate B 7 pKi 100 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of human recombinant Abl B 7.36 pKi 44 nM Ki Bioorg Med Chem Lett (2008) 18: 1207-1211 [PMID:18078752]
GtoPdb - - 7.36 pKi 44 nM Ki Bioorg Med Chem Lett (2008) 18: 1207-11 [PMID:18078752];
Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of histidine-tagged human recombinant SRC expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using ATP as substrate B 6.26 pKi 550 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of histidine-tagged human recombinant SRC expressed in baculovirus system assessed as [gamma32P]ATP utilization after 10 mins by liquid scintillation counting using KVEKIGEGTYGVVYK as substrate B 6.26 pKi 550 nM Ki Bioorg Med Chem (2010) 18: 3999-4008 [PMID:20451394]
ChEMBL Inhibition of recombinant human c-Src B 6.45 pKi 354 nM Ki Bioorg Med Chem Lett (2008) 18: 1207-1211 [PMID:18078752]

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]