ChEMBL ligand: CHEMBL4114766 (Atuzabrutinib, PRN-473, PRN473, SAR-444727, SAR444727)
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] There should be some charts here, you may need to enable JavaScript!
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] There should be some charts here, you may need to enable JavaScript!
BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] There should be some charts here, you may need to enable JavaScript!
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!
tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] There should be some charts here, you may need to enable JavaScript!
TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] There should be some charts here, you may need to enable JavaScript!

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 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]