compound 30 [PMID: 21757343] [Ligand Id: 6407] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1808901
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor in Rat [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]
GtoPdb - - 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2011) 21: 4891-9 [PMID:21757343]
ChEMBL Displacement of [3H]-MPEP from human mGluR5 expressed in CHO cells after 60 mins B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2011) 21: 4891-4899 [PMID:21757343]
ChEMBL Negative allosteric modulation of human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization after 1 hr by FLIPR assay F 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-4899 [PMID:21757343]
GtoPdb - - 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-9 [PMID:21757343]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2011) 21: 4891-9 [PMID:21757343]

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]