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 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]