CGI1746 [Ligand Id: 8066] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1230541 |
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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 C481S mutant (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2022) 229: 114009-114009 [PMID:34839996] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Eur J Med Chem (2022) 229: 114009-114009 [PMID:34839996] |
| 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 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]
