compound 11s [PMID: 19433355] [Ligand Id: 6215] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1783876
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO-K1 cells by whole cell patch-clamp assay B 4.51 pIC50 31000 nM IC50 Eur J Med Chem (2014) 85: 629-637 [PMID:25127154]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay F 8.17 pIC50 6.7 nM IC50 Eur J Med Chem (2014) 85: 629-637 [PMID:25127154]
ChEMBL Antagonist activity at human mGluR1 F 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]
GtoPdb - - 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-203 [PMID:19433355]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 8.33 pKi 4.7 nM Ki Bioorg Med Chem Lett (2009) 19: 3199-203 [PMID:19433355]
ChEMBL Antagonist activity at rat mGluR1 F 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Antagonist activity at human mGluR5 F 5.52 pIC50 >3000 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]

ChEMBL data shown on this page come from version 32:

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]