CPPHA [Ligand Id: 1423] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL366217 |
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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 | Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1082-1086 [PMID:27994742] |
| GtoPdb | - | - | 6.3 | pIC50 | - | - | - | J Pharmacol Exp Ther (2004) 309: 568-77 [PMID:14747613] |
| ChEMBL | Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2004) 47: 5825-5828 [PMID:15537338] |
| ChEMBL | Activity at human mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay | B | 6.6 | pEC50 | 250 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1386-1391 [PMID:17210250] |
| ChEMBL | Positive allosteric modulation of human mGluR5 | B | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Displacement of [3H]-MethoxyPEPy from mGlu5 receptor in primary rat astrocytes after 8 hrs by micro beta scintillation counting analysis | B | 6.03 | pIC50 | 930 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1082-1086 [PMID:27994742] |
| ChEMBL | Activity at rat mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay | B | 6 | pEC50 | <1000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1386-1391 [PMID:17210250] |
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]
