PD173074 [Ligand Id: 5037] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189584 (PD-173074)
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
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  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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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 Cellular target engagement assay with: FGFR1 B 7.58 pIC50 26.2 nM IC50 null
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 FGFR1 (unknown origin) B 7.67 pIC50 21.5 nM IC50 Eur J Med Chem (2021) 210: 112990-112990 [PMID:33199155]
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 Cellular target engagement assay with: FGFR2 B 7.6 pIC50 25.1 nM IC50 null
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 Cellular target engagement assay with: FGFR3 B 7.23 pIC50 58.4 nM IC50 null
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]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Cellular target engagement assay with: FGFR4 B 5.8 pIC50 1579 nM IC50 null
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 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]