Ro0711401 [Ligand Id: 6204] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL521982
  • 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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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]
ChEMBL Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins F 6.61 pEC50 246 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
ChEMBL Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins F 6.61 pEC50 245.47 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
ChEMBL Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM) B 6.85 pEC50 141.3 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
ChEMBL Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit) B 6.85 pEC50 141.25 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization F 6.56 pEC50 276.5 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
ChEMBL Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization F 6.56 pEC50 275.42 nM EC50 Bioorg Med Chem Lett (2016) 26: 2289-2292 [PMID:27013388]
ChEMBL Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology F 6.69 pEC50 202 nM EC50 Bioorg Med Chem Lett (2009) 19: 1666-1669 [PMID:19233648]
GtoPdb - - 7.25 pEC50 56 nM EC50 Bioorg Med Chem Lett (2009) 19: 1666-9 [PMID:19233648]
ChEMBL Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay F 7.25 pEC50 56 nM EC50 Bioorg Med Chem Lett (2009) 19: 1666-1669 [PMID:19233648]

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]