4-MPPTS [Ligand Id: 1402] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL108939 (LY-487379)
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Ability to displace [3H]LY-341,495 at glutamate-site on Metabotropic glutamate receptor 2; No significant displacement B 4 pIC50 >100000 nM IC50 J Med Chem (2003) 46: 3189-3192 [PMID:12852748]
GtoPdb - - 5.8 pIC50 - - - J Med Chem (2003) 46: 3189-92 [PMID:12852748];
Mol Pharmacol (2003) 64: 798-810 [PMID:14500736];
Psychopharmacology (Berl.) (2005) 179: 271-83 [PMID:15717213];
Bioorg Med Chem Lett (2004) 14: 3099-102 [PMID:15149652]
ChEMBL Binding affinity towards human metabotropic glutamate receptor 2 determined by [35S]GTP gamma S binding assay F 5.77 pEC50 1700 nM EC50 Bioorg Med Chem Lett (2004) 14: 5867-5872 [PMID:15501058]
ChEMBL Effective concentration for binding to human metabotropic glutamate receptor 2 as determined by GTPgammaS assay B 5.77 pEC50 1700 nM EC50 Bioorg Med Chem Lett (2004) 14: 5329-5332 [PMID:15454221]
ChEMBL Effective concentration against Metabotropic glutamate receptor 2 B 6.57 pEC50 270 nM EC50 J Med Chem (2003) 46: 3189-3192 [PMID:12852748]

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]