atuzabrutinib [Ligand Id: 11666] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4114766 (Atuzabrutinib, PRN-473, PRN473, SAR-444727, SAR444727) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 6.43 | pIC50 | 368 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of ERBB2 (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 5.97 | pIC50 | 1081 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Inhibition of ERBB4 (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| 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 by caliper electrophoresis method | B | 8.66 | pIC50 | 2.2 | 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 by caliper electrophoresis method | B | 8.74 | pIC50 | 1.8 | 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] | ||||||||
| ChEMBL | Inhibition of biotinylated-labeled BTK-selective probe binding to BTK in human Ramos assessed as target occupancy pretreated for 1 hr followed by probe addition measured for 18 hrs by AlphaScreen assay | B | 7.52 | pIC50 | 30.1 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| ChEMBL | Enzymatic Activity Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula (IA), (I′) or (I). Serial dilutions of test compounds were incubated with human recombinant Btk (2 nM), ATP (40 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). Percent inhibition was calculated for each compound dilution and the concentration that produced 50% inhibition was calculated. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-9090621-B2. Tyrosine kinase inhibitors (2015) |
| GtoPdb | Determined in a biochemical enzyme assay measuring inhibition of peptide substrate FAM-GEEPLYWSFPAKKK-NH2 phosphorylation | - | 8.7 | pIC50 | 2 | nM | IC50 | US9090621B2. Tyrosine kinase inhibitors (2015) |
| ChEMBL | Inhibition of BTK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
| ChEMBL | Inhibition of ITK (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 6.52 | pIC50 | 303 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method | B | 5.3 | pIC50 | >5000 | 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 by caliper electrophoresis method | B | 8.72 | pIC50 | 1.9 | 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 by caliper electrophoresis method | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2022) 65: 5300-5316 [PMID:35302767] |
ChEMBL data shown on this page come from version 35:
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]
