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ChEMBL ligand: CHEMBL190270 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.6 | pKi | 250 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7381-7384 [PMID:21067920] |
ChEMBL | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | F | 6.75 | pEC50 | 177.83 | nM | EC50 | J Med Chem (2013) 56: 7243-7259 [PMID:23947773] |
ChEMBL | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | F | 6.75 | pEC50 | 176 | nM | EC50 | J Med Chem (2013) 56: 7243-7259 [PMID:23947773] |
ChEMBL | Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay | F | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
GtoPdb | - | - | 8 | pEC50 | - | - | - |
J Pharmacol Exp Ther (2005) 313: 199-206 [PMID:15608073]; J Med Chem (2004) 47: 5825-8 [PMID:15537338] |
ChEMBL | Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2004) 47: 5825-5828 [PMID:15537338] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
ChEMBL | Displacement of [3H]methoxyPEPy from rat mGluR5 expressed in HEK293 cells | B | 5.42 | pKi | 3760 | nM | Ki | J Med Chem (2006) 49: 3332-3344 [PMID:16722652] |
ChEMBL | Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay | F | 7.01 | pEC50 | 98 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
ChEMBL | Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes | F | 7.11 | pEC50 | 77 | nM | EC50 | J Med Chem (2006) 49: 3332-3344 [PMID:16722652] |
ChEMBL | Effective concentration against metabotropic glutamate receptor 5 of rat | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2004) 47: 5825-5828 [PMID:15537338] |
GtoPdb | - | - | 7.7 | pEC50 | - | - | - | J Med Chem (2004) 47: 5825-8 [PMID:15537338] |
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]