ChEMBL ligand: CHEMBL3936761 (Bgb-3111, BGB-3111, Brukinsa, Zanubrutinib)
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!
Platelet glycoprotein VI (GPVI) in Human [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6] 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!

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 GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hrs by ELISA	B	7.42	pIC50	38.3	nM	IC50	J Med Chem (2022) 65: 2694-2709 [PMID:35099969]
ChEMBL	Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	7.67	pIC50	21.2	nM	IC50	J Med Chem (2021) 64: 16242-16270 [PMID:34672559]
ChEMBL	Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2021) 225: 113724-113724 [PMID:34391034]
Platelet glycoprotein VI (GPVI) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6]
ChEMBL	Inhibition of GP6 in human whole blood assessed as protein-mediated platelet aggregation preincubated for 15 mins followed by collagen stimulation and measured for 10 mins by multiple electrode aggregometry	B	6.29	pIC50	510	nM	IC50	J Med Chem (2020) 63: 12213-12242 [PMID:32463237]
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL	Inhibition of N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	7.94	pIC50	11.5	nM	IC50	Eur J Med Chem (2021) 225: 113724-113724 [PMID:34391034]
ChEMBL	Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	8.27	pIC50	5.4	nM	IC50	J Med Chem (2021) 64: 16242-16270 [PMID:34672559]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL	Inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA	B	8.46	pIC50	3.5	nM	IC50	J Med Chem (2022) 65: 2694-2709 [PMID:35099969]
ChEMBL	Inhibition of full-length N-terminal GST tagged BTK (1 to 659 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	8.66	pIC50	2.2	nM	IC50	Eur J Med Chem (2021) 225: 113724-113724 [PMID:34391034]
ChEMBL	Inhibition of full-length N-terminal GST tagged BTK (2 to 659 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2021) 64: 16242-16270 [PMID:34672559]
ChEMBL	Time-Resolved Fluorescence Resonance Energy Transfer Assay: Compounds disclosed herein were tested for inhibition of Btk kinase activity in an assay based on time-resolved fluorescence resonance energy transfer methodology. Recombinant Btk was pre-incubated with the compounds disclosed herein at room temperature for 1 hour in an assay buffer containing 50 mM Tris pH7.4, 10 mM MgCl2, 2 mM MnCl2, 0.1 mM EDTA, 1 mM DT, 20 nM SEB, 0.1% BSA, 0.005% tween-20. The reactions were initiated by the addition of ATP (at the concentration of ATP Km) and peptide substrate (Biotin-AVLESEEELYSSARQ-NH2). After incubating at room temperature for 1 h, an equal volume of stop solution containing 50 mM HEPES pH7.0, 800 mM KF, 20 mM EDTA, 0.1% BSA, Eu cryptate-conjugated p-Tyr66 antibody and streptavidin-labeled XL665 was added to stop the reaction. Plates were further incubated at room temperature for 1 hour, and then the TR-FRET signals (ex337 nm, em 620 nm/665 nm) were read on BMG PHERAstar FS instrument. The residual enzyme activity in presence of increasing concentrations of compounds was calculated based on the ratio of fluorescence at 615 nm to that at 665 nm. The IC50 for each compound was derived from fitting the data to the four-parameter logistic equation by Graphpad Prism software.	B	8.7	pIC50	2	nM	IC50	US-9447106-B2. Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators (2016)
GtoPdb	Inhibition of the enzymatic activity of recombinant human BTK in a TR-FRET assay.	-	8.7	pIC50	2	nM	IC50	US9447106B2. Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators. (2016)
ChEMBL	Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay	B	8.74	pIC50	1.8	nM	IC50	J Med Chem (2019) 62: 7923-7940 [PMID:31381333]
ChEMBL	Inhibition of human BTK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method	B	9.04	pIC50	0.92	nM	IC50	J Med Chem (2019) 62: 7923-7940 [PMID:31381333]
ChEMBL	Inhibition of N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2019) 62: 7923-7940 [PMID:31381333]
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 N-terminal GST-tagged ITK (2 to 620 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	6.69	pIC50	202.9	nM	IC50	Eur J Med Chem (2021) 225: 113724-113724 [PMID:34391034]
ChEMBL	Inhibition of full-length N-terminal GST-tagged ITK (2 to 620 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	B	7.18	pIC50	65.9	nM	IC50	J Med Chem (2021) 64: 16242-16270 [PMID:34672559]

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]