ChEMBL ligand: CHEMBL3290142
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 recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay	B	7.14	pIC50	72	nM	IC50	Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL	Inhibition of EGFR (unknown origin) after 1 hr by HTRF assay	B	7.96	pIC50	11	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
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 HER2 (unknown origin) after 1 hr by HTRF assay	B	7.72	pIC50	19	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
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 HER4 (unknown origin) after 1 hr by HTRF assay	B	8.26	pIC50	5.5	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
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 wild type N-terminal GST tagged BLK (unknown origin) (1 to 505 residues) expressed in sf21 insect cell using TK as substrate incubated for 50 mins in presence of ATP by HTRF assay	B	7.73	pIC50	18.8	nM	IC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
ChEMBL	Inhibition of (S)-3-(3-(5-acrylamido-6-(3-(5-(2-methyl-5-(3-(trifluoromethyl)benzamido)benzamido)pyrimidin-2-ylamino)phenylamino)-6-oxohexylamino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:1',2'-f][1,3,2]diazaborinin-4-ium-5-uide binding to BLK in human NAMALVA cells preincubated for 1 hr followed by compound washout for three times and treated with probe for 1 hr by competitive labeling assay	B	7.82	pIC50	15	nM	IC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
ChEMBL	Inhibition of Blk (unknown origin) after 1 hr by HTRF assay	B	8.57	pIC50	2.7	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb	-	-	8.57	pIC50	2.7	nM	IC50	J Med Chem (2014) 57: 5112-28 [PMID:24915291]
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL	Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay	B	7.62	pIC50	24	nM	IC50	Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
GtoPdb	-	-	8.72	pIC50	1.9	nM	IC50	J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL	Inhibition of Bmx (unknown origin) after 1 hr by HTRF assay	B	8.72	pIC50	1.9	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL	Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay	B	7.57	pKi	27.2	nM	Ki	Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL	Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay	B	7.6	pIC50	25	nM	IC50	Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL	Inhibition of wild type N-terminal GST tagged BTK (unknown origin) (2 to 659 residues) expressed in sf21 insect cell using TK as substrate incubated for 50 mins in presence of ATP by HTRF assay	B	7.69	pIC50	20.5	nM	IC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
ChEMBL	Inhibition of (S)-3-(3-(5-acrylamido-6-(3-(5-(2-methyl-5-(3-(trifluoromethyl)benzamido)benzamido)pyrimidin-2-ylamino)phenylamino)-6-oxohexylamino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:1',2'-f][1,3,2]diazaborinin-4-ium-5-uide binding to BTK in human NAMALVA cells preincubated for 1 hr followed by compound washout for three times and treated with probe for 1 hr by competitive labeling assay	B	7.74	pIC50	18	nM	IC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
ChEMBL	Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis	B	7.85	pIC50	14	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
ChEMBL	Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis	B	8.07	pIC50	8.5	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
ChEMBL	Inhibition of Btk (unknown origin) after 1 hr by HTRF assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb	-	-	8.36	pIC50	5	nM	IC50	J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL	Inhibition of BTK in goat anti-human IgM antibody stimulated human Ramos cells assessed as PLCgamma2 phosphorylation preincubated for 1 hr followed by antibody stimulation by Western blot analysis	B	7.62	pEC50	24	nM	EC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
ChEMBL	Inhibition of BTK in goat anti-human IgM antibody stimulated human Ramos cells assessed as BTK autophosphorylation at Tyr233 residue preincubated for 1 hr followed by antibody stimulation by Western blot analysis	B	7.74	pEC50	18	nM	EC50	Eur J Med Chem (2022) 229: 114051-114051 [PMID:34952433]
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) after 1 hr by HTRF assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
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) after 1 hr by HTRF assay	B	5.57	pIC50	2680	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
ChEMBL	Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay	B	5.77	pIC50	1705	nM	IC50	Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
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) after 1 hr by HTRF assay	B	8.09	pIC50	8.2	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb	-	-	8.09	pIC50	8.2	nM	IC50	J Med Chem (2014) 57: 5112-28 [PMID:24915291]
TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681]
GtoPdb	-	-	8.72	pIC50	1.9	nM	IC50	J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL	Inhibition of Rlk (unknown origin) after 1 hr by HTRF assay	B	8.72	pIC50	1.9	nM	IC50	J Med Chem (2014) 57: 5112-5128 [PMID:24915291]

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]