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 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]
