CGI1746 [Ligand Id: 8066] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1230541
  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Mouse [ChEMBL: CHEMBL3259478] [GtoPdb: 1948] [UniProtKB: P35991]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of biotinylated and activated BTK (unknown origin) using FITC-labeled Srctide peptide substrate and ATP B 7.09 pIC50 81 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2033-2036 [PMID:25872980]
ChEMBL Inhibition of BTK (unknown origin) B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1333-1337 [PMID:25701252]
GtoPdb - - 8.72 pIC50 1.9 nM IC50 Nat Chem Biol (2011) 7: 41-50 [PMID:21113169]
ChEMBL Inhibition of BTK (unknown origin) B 8.72 pIC50 1.9 nM IC50 Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
ChEMBL Inhibition of biotinylated and unactivated BTK (unknown origin) using FITC-labeled Srctide peptide substrate and ATP B 9.21 pIC50 0.61 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2033-2036 [PMID:25872980]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259478] [GtoPdb: 1948] [UniProtKB: P35991]
ChEMBL Inhibition of BTK-mediated CD86 surface expression in Balb/c mouse splenocytes preincubated for 60 mins before F(ab')2 anti-mouse IgM measured after 24 hrs by flow cytometry B 6.82 pIC50 150 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1333-1337 [PMID:25701252]

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]