Ro0711401 [Ligand Id: 6204] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL521982 |
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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 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]
