Ro4491533 [Ligand Id: 6226] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1629855 (Ro-4491533) |
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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] | ||||||||
| GtoPdb | - | - | 8.21 | pKi | 6.2 | nM | Ki | J Neurogenet (2011) 25: 152-66 [PMID:22091727] |
| ChEMBL | Negative allosteric modulation of mGlu2 by cell-based assay | B | 6.53 | pIC50 | 296 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673] |
| ChEMBL | Negative allosteric modulation of mGlu2 receptor (unknown origin) | B | 6.53 | pIC50 | 296 | nM | IC50 | J Med Chem (2013) 56: 5208-5212 [PMID:23718281] |
| GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-74 [PMID:20971004] |
| ChEMBL | Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-6974 [PMID:20971004] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| GtoPdb | - | - | 8.27 | pKi | 5.4 | nM | Ki | J Neurogenet (2011) 25: 152-66 [PMID:22091727] |
| ChEMBL | Antagonist activity at rat mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current | F | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-6974 [PMID:20971004] |
| ChEMBL | Antagonist activity at recombinant rat mGluR2 expressed in forskolin-stimulated CHO cells assessed as inhibition of (1S,3R)-ACPD induced cAMP production | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-6974 [PMID:20971004] |
| ChEMBL | Partial displacement of [3H]LY354740 from recombinant rat mGluR2 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-6974 [PMID:20971004] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 |
Bioorg Med Chem Lett (2010) 20: 6969-74 [PMID:20971004]; J Neurogenet (2011) 25: 152-66 [PMID:22091727] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| ChEMBL | Negative allosteric modulation of mGlu3 by cell-based assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673] |
| ChEMBL | Negative allosteric modulation of mGlu3 receptor (unknown origin) | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2013) 56: 5208-5212 [PMID:23718281] |
| GtoPdb | - | - | 6.6 | pIC50 | 270 | nM | IC50 | J Neurogenet (2011) 25: 152-66 [PMID:22091727] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| GtoPdb | - | - | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-74 [PMID:20971004] |
| ChEMBL | Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current | F | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6969-6974 [PMID:20971004] |
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]
