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 |
|---|---|---|---|---|---|---|---|---|
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of BLK (unknown origin) using peptide substrate in presence of ATP | B | 8.2 | pIC50 | 6.3 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| 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 | Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| ChEMBL | Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Inhibition of TEC (unknown origin) using peptide substrate in presence of ATP | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] | ||||||||
| ChEMBL | Inhibition of RLK (unknown origin) using peptide substrate in presence of ATP | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
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]
