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ChEMBL ligand: CHEMBL3290142 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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 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] |
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 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]