PD 158780 [Ligand Id: 6015] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL53753 (PD-158780)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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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 EGF-dependent autophosphorylation of EGF-R in A431 cells F 4.89 pIC50 13000 nM IC50 J. Med. Chem. (1998) 41: 742-751 [PMID:9513602]
GtoPdb Inhibition of EGFR autophosphorylation - 7.82 pIC50 15 nM IC50 J Med Chem (1997) 40: 1820-6 [PMID:9191958]
ChEMBL Tested for inhibition of autophosphorylation in Epidermal growth factor receptor stimulated A431 cells F 7.82 pIC50 15 nM IC50 J. Med. Chem. (1997) 40: 1820-1826 [PMID:9191958]
ChEMBL Inhibition of Epidermal growth factor receptor autophosphorylation in A431 human epidermoid carcinoma cells B 7.82 pIC50 15 nM IC50 J. Med. Chem. (1996) 39: 1823-1835 [PMID:8627606]
ChEMBL Inhibition of autophosphorylation of epidermal growth factor receptor in A431 cells in culture F 7.89 pIC50 13 nM IC50 J. Med. Chem. (1998) 41: 742-751 [PMID:9513602]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of MNK1 B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (2010) 53: 6618-6628 [PMID:20722422]
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 heregulin-dependent autophosphorylation of ErbB2 receptor in MDA-MB-453 cells F 4.28 pIC50 52000 nM IC50 J. Med. Chem. (1998) 41: 742-751 [PMID:9513602]

ChEMBL data shown on this page come from version 31:

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]