VU0360172 [Ligand Id: 6400] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1684242 (VU0360172)
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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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 Positive allosteric modulation of mGlu5 receptor assessed as calcium mobilization F 7.8 pEC50 16 nM EC50 Bioorg Med Chem Lett (2011) 21: 1350-1353 [PMID:21315585]
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 human HEK293 cells after 1 hr by scintillation counter B 6.71 pKi 195 nM Ki Bioorg Med Chem Lett (2012) 22: 6481-6485 [PMID:22981332]
GtoPdb - - 6.71 pKi 195 nM Ki Mol Pharmacol (2010) 78: 1105-23 [PMID:20923853]
ChEMBL Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as calcium mobilization F 7.41 pEC50 39 nM EC50 J Med Chem (2013) 56: 7976-7996 [PMID:24050755]
ChEMBL Positive allosteric modulation of rat mGluR5 expressed in human HEK293 cells assessed as calcium mobilization F 7.8 pEC50 16 nM EC50 Bioorg Med Chem Lett (2012) 22: 6481-6485 [PMID:22981332]
GtoPdb - - 7.8 pEC50 16 nM EC50 Mol Pharmacol (2010) 78: 1105-23 [PMID:20923853]

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]