rilzabrutinib [Ligand Id: 9993] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3702854 (Prn-1008, Prn1008, PRN1008, Rilzabrutinib) |
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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] | ||||||||
| GtoPdb | Measured in a caliper-based kinase assay, to assess inhibition of recombinant human BTK kinase activity (@ 16 μM ATP) using the phosphoacceptor peptide substrate FAM-GEEPLYWSFPAKKK-NH2. | - | 8.82 | pIC50 | 1.5 | nM | IC50 | WO2014039899. PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS (2014) |
| ChEMBL | Caliper-Based Kinase Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of the present disclosure. Serial dilutions of test compounds were incubated with human recombinant Btk (0.5 nM), ATP (16 μM) and a phosphoacceptor peptide substrate FAM-GEEPLYWSFPAKKK-NH2 (1 μM) at room temperature for 3 h. The reaction was then terminated with EDTA, final concentration 20 mM and the phosphorylated reaction product was quantified on a Caliper Desktop Profiler (Caliper LabChip 3000). | B | 8.82 | pIC50 | 1.5 | nM | IC50 | US-9266895-B2. Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors (2016) |
| ChEMBL | Inhibition of BTK (unknown origin) One-hour enzymatic assay without pre-incubation | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659] |
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]
