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 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]
