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 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]
