SU5402 [Ligand Id: 11743] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL89363 (SU-5402) |
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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 | Evaluated for inhibitory activity towards tyrosine kinase Epidermal growth factor receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against Epidermal growth factor receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Epidermal growth factor receptor (EGF RTK). | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| ChEMBL | Inhibitory activity against ligand-dependent EGF cell proliferation | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| 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 bFGF-mediated tyrosine phosphorylation | F | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2000) 43: 4200-4211 [PMID:11063616] |
| ChEMBL | Inhibition of FGFR1K autophosphorylation activity assessed as [32P] incorporation | B | 5 | pIC50 | 10000 | nM | IC50 | Science (1997) 276: 955-960 [PMID:9139660] |
| ChEMBL | Inhibition of FGFR1 kinase domain (unknown origin) | B | 5 | pIC50 | 10000 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibitory activity of compound against FGF induced cell proliferation | F | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Inhibition of FGFR1 using poly(Glu-Tyr)4:1 as substrate after 60 mins by ELISA | B | 6.48 | pIC50 | 334 | nM | IC50 | J Med Chem (2011) 54: 3732-3745 [PMID:21517068] |
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1999) 42: 5120-30 [PMID:10602697] |
| ChEMBL | Evaluated for inhibitory activity towards Fibroblast growth factor receptor 1 | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against Fibroblast growth factor receptor 1 | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| 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 acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting | B | 5 | pIC50 | 10000 | nM | IC50 | Science (1997) 276: 955-960 [PMID:9139660] |
| ChEMBL | Inhibition of FGF induced FGFR1 autophosphorylation in mouse NIH 3T3 cells preincubated for 5 mins followed by FGF-stimulation for 5 mins in presence of [gamma-32P]ATP by SDS-PAGE based autoradiography | B | 5 | pIC50 | 10000 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Insulin-like growth factor I receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Test concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Platelet-derived growth factor receptor beta (PDGF RTK). | B | 4.22 | pIC50 | 60900 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| ChEMBL | Inhibitory activity of compound against PDGF induced cell proliferation | F | 4.55 | pIC50 | 28400 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| GtoPdb | - | - | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (1999) 42: 5120-30 [PMID:10602697] |
| ChEMBL | Evaluated for inhibitory activity towards tyrosine kinase PDGF-Rbeta | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against Platelet-derived growth factor receptor beta | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| 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 | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Her-2 receptor tyrosine kinase (HER-2 RTK) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Evaluated for inhibitory activity towards p60 c-Src tyrosine kinase | B | 4.97 | pIC50 | 10600 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3516] [GtoPdb: 1812] [UniProtKB: P35969] | ||||||||
| ChEMBL | Concentration required to achieve 50% inhibition of tyrosine phosphorylation on murine VEGF receptor (FLK-1 RTK). | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1998) 41: 2588-2603 [PMID:9651163] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibitory activity of compound against VEGF induced cell proliferation | F | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Evaluated for inhibitory activity towards tyrosine kinase Vascular endothelial growth factor receptor 2 | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2000) 43: 2655-2663 [PMID:10893303] |
| ChEMBL | Inhibitory activity against Vascular endothelial growth factor receptor 2 | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1999) 42: 5120-5130 [PMID:10602697] |
| ChEMBL | Inhibition of KDR | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2126-2133 [PMID:17306530] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1999) 42: 5120-30 [PMID:10602697] |
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]
