CNX-774 [Ligand Id: 9266] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2216827
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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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 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 6.13 pIC50 737 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
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 5 pIC50 >10000 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
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 6.68 pKi 209.2 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 8.02 pIC50 9.5 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
GtoPdb - - 9 pIC50 <1 nM IC50 J Med Chem (2012) 55: 6243-62 [PMID:22621397]
ChEMBL Inhibition of Btk in human Ramos cells B 9 pIC50 1 nM IC50 J. Med. Chem. (2012) 55: 6243-6262 [PMID:22621397]
ChEMBL Inhibition of Btk B 9 pIC50 <1 nM IC50 J. Med. Chem. (2012) 55: 6243-6262 [PMID:22621397]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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 5.81 pIC50 1533 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]