compound 2f [PMID: 17532216] [Ligand Id: 6342] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL245990
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
GtoPdb - - 6.9 pKi 127 nM Ki Bioorg Med Chem Lett (2007) 17: 4303-7 [PMID:17532216]
ChEMBL Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay F 5.85 pIC50 1412 nM IC50 Bioorg Med Chem Lett (2007) 17: 4303-4307 [PMID:17532216]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Antagonist activity at human mGluR5 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay F 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2007) 17: 4303-4307 [PMID:17532216]

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]