compound 8 [PMID: 15482908] [Ligand Id: 6448] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL187107 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Inhibitory concentration towards human glutamate receptor 5 in calcium flux assay | F | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2004) 47: 4645-4648 [PMID:15341479] |
| ChEMBL | Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist | F | 8.41 | pIC50 | 3.9 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5473-5476 [PMID:15482906] |
| GtoPdb | - | - | 8.41 | pIC50 | 3.9 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5481-4 [PMID:15482908] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5481-4 [PMID:15482908] |
| ChEMBL | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5481-5484 [PMID:15482908] |
| ChEMBL | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5473-5476 [PMID:15482906] |
| ChEMBL | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5477-5480 [PMID:15482907] |
| ChEMBL | Ability to displace [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from binding to metabotropic glutamate receptor 5 in rat cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 5061-5064 [PMID:16183275] |
| ChEMBL | Displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from glutamate 5 receptor of rat cortical membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2004) 47: 4645-4648 [PMID:15341479] |
| ChEMBL | Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5477-5480 [PMID:15482907] |
| ChEMBL | In vitro functional activity measured by changes in cytosolic [Ca2+] concentrations against rat metabotropic glutamate receptor 5 | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5061-5064 [PMID:16183275] |
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]
