CPPZ [Ligand Id: 6416] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1289113 |
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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]-MPEP from human mGluR5 | B | 5.63 | pKi | 2370 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920] |
| ChEMBL | Positive allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as Ca2+ influx by FLIPR assay | F | 6.26 | pEC50 | 550 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920] |
| ChEMBL | Positive allosteric modulation of human mGluR5 over-expressed in HEK293 cells | B | 6.26 | pEC50 | 550 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
| GtoPdb | - | - | 6.3 | pEC50 | 500 | nM | EC50 | Eur J Pharmacol (2011) 659: 146-54 [PMID:21335002] |
| mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 5.51 | pKi | 3100 | nM | Ki | Eur J Pharmacol (2011) 659: 146-54 [PMID:21335002] |
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]
