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ChEMBL ligand: CHEMBL381055 (ADX-47273) |
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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 | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | F | 6.7 | pEC50 | 199.53 | 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 | 6.7 | pEC50 | 199 | nM | EC50 | J Med Chem (2013) 56: 7243-7259 [PMID:23947773] |
GtoPdb | - | - | 6.8 | pEC50 | 157 | nM | EC50 | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
ChEMBL | Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay | F | 6.8 | pEC50 | 157 | 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] | ||||||||
GtoPdb | - | - | 5.44 | pKi | 3650 | nM | Ki | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Neuropharmacology (2005) 49 (S1): 252- |
ChEMBL | Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes | F | 6.77 | pEC50 | 170 | nM | EC50 | J Med Chem (2006) 49: 3332-3344 [PMID:16722652] |
ChEMBL | Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2013) 56: 7976-7996 [PMID:24050755] |
GtoPdb | - | - | 7.26 | pEC50 | 55 | nM | EC50 | Neuropharmacology (2013) 64: 224-39 [PMID:22884720] |
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]