PD173074 [Ligand Id: 5037] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189584 (PD-173074) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Inhibition of MEK1 fused with GST by autoradiography | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2012) 55: 5003-5012 [PMID:22612866] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR | B | 4.3 | pIC50 | >50000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of FGFR1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| ChEMBL | Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by human fibroblast growth factor receptor 1 | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2005) 48: 4628-4653 [PMID:16000000] |
| ChEMBL | Inhibition of FGFR1 | B | 7.67 | pIC50 | 21.5 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of recombinant full length human FGFR1 expressed in baculovirus infected insect cells in presence of [gamma-32P]ATP after 10 mins by scintillation counting based radioactive filter binding assay | B | 7.67 | pIC50 | 21.5 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibition of full length human FGFR1 expressed in baculovirus system using poly (Glu,Tyr)4:1 as substrate incubated for 10 mins in presence of [gamma-32P]ATP by scintillation counting analysis | B | 7.67 | pIC50 | 21.5 | nM | IC50 | ACS Med Chem Lett (2016) 7: 629-634 [PMID:27326339] |
| ChEMBL | Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by human FGFR1 in DELFIA assay | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2005) 48: 4628-4653 [PMID:16000000] |
| ChEMBL | Inhibition of FGFR1 by cellular assay | B | 7.68 | pEC50 | 21 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Inhibition of FGFR3 by cellular assay | B | 7.52 | pEC50 | 30 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of InsR | B | 4.3 | pIC50 | >50000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| ChEMBL | Inhibition of INSR | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2012) 55: 5003-5012 [PMID:22612866] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622] | ||||||||
| ChEMBL | Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by mouse platelet-derived growth factor receptor-beta | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2005) 48: 4628-4653 [PMID:16000000] |
| ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
| ChEMBL | Inhibition of ATM | B | 4.75 | pIC50 | 17600 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of cSrc | B | 4.7 | pIC50 | 19800 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Tyrosine-protein kinase SRC in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523] | ||||||||
| ChEMBL | Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by avian c-Src tyrosine kinase | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2005) 48: 4628-4653 [PMID:16000000] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of Src | B | 4.7 | pIC50 | 20000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by human VEGFR 2 in DELFIA assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2005) 48: 4628-4653 [PMID:16000000] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) overexpressed in mouse NIH/ 3T3 cells incubated for 5 mins followed by stimulation with VEGF for 5 mins by immunoblotting analysis | B | 7 | pIC50 | 100 | nM | IC50 | ACS Med Chem Lett (2016) 7: 629-634 [PMID:27326339] |
| ChEMBL | Inhibition of VEGFR2 by cellular assay | B | 6.6 | pEC50 | 250 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 19936-19941 [PMID:18077425] |
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]
