GDC-0834 [Ligand Id: 9263] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2057915 |
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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 BTK (unknown origin) by Lanthascreen assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 575-579 [PMID:26675441] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1333-7 [PMID:25701252] |
| ChEMBL | Inhibition of BTK (unknown origin) by Lanthascreen method | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1333-1337 [PMID:25701252] |
| ChEMBL | Inhibition of human BTK by enzymatic assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| ChEMBL | Inhibition of BTK in human whole blood B-cells assessed as inhibition of both anti-IgD-stimulated CD69 expression | B | 6.42 | pEC50 | 380 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 1333-1337 [PMID:25701252] |
| ChEMBL | Inhibition of BTK in human whole blood basophils assessed as inhibition of both anti-IgE-stimulated CD63 expression | B | 6.46 | pEC50 | 350 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 1333-1337 [PMID:25701252] |
| 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 | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1333-1337 [PMID:25701252] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
