PD173074 [Ligand Id: 5037] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189584 |
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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 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] |
| ChEMBL | Inhibition of EGFR (unknown origin) in presence of ATP | B | 4.3 | pIC50 | >50000 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | ATP-competitive inhibition of FGFR1 (unknown origin) in presence of ATP | B | 7.34 | pKi | 45.2 | nM | Ki | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| ChEMBL | ATP-competitive inhibition of FGFR1 cytoplasmic domain (unknown origin) in presence of ATP | B | 7.44 | pKi | 36.4 | nM | Ki | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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 FGFR1 cytoplasmic domain (unknown origin) in presence of ATP | B | 7.54 | pIC50 | 28.9 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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 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 FGFR1 | B | 7.67 | pIC50 | 21.5 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Affinity Biochemical interaction: (Enzymatic inhibition assay (5 uM ATP)) EUB0000699a FGFR1 | B | 7.67 | pIC50 | 21.5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of FGFR1 (unknown origin) in presence of ATP | B | 7.67 | pIC50 | 21.5 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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 | Affinity On-target Cellular interaction: (Immunoblotting (inhibition of FGFR1 autophosphorylation in NIH 3T3 cells)) EUB0000699a FGFR1 | B | 7.82 | pIC50 | 15 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| 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 1/Fibroblast growth factor receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3960] [GtoPdb: 1808] [UniProtKB: P16092] | ||||||||
| ChEMBL | Inhibition of FGFR1 autophosphorylation in mouse NIH/3T3 cells assessed as reduction in aFGF and heparin-induced autophosphorylation incubated for 5 mins before stimulation for 5 mins with aFGF and heparin by SDS-PAGE and immunoblot method | B | 9 | pIC50 | 1 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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] |
| ChEMBL | Inhibition of INSR (unknown origin) in presence of ATP | B | 4.3 | pIC50 | >50000 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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] |
| Proto-oncogene 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/Proto-oncogene 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] |
| ChEMBL | Inhibition of c-SRC (unknown origin) in presence of ATP | B | 4.7 | pIC50 | 19800 | nM | IC50 | EMBO J (1998) 17: 5896-5904 [PMID:9774334] |
| 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] |
| 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 36:
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]
