MGS0039 [Ligand Id: 1397] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL186453 |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells | B | 4.03 | pIC50 | 93300 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Binding affinity to mGLUR2 | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| ChEMBL | Antagonist activity at mGLUR2 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production | F | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 8.62 | pKi | 2.38 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Neuropharmacology (2004) 46: 457-67 [PMID:14975669]; J Med Chem (2004) 47: 4570-87 [PMID:15317467] |
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| ChEMBL | Binding affinity to mGLUR3 | B | 8.35 | pKi | 4.5 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| ChEMBL | Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production | F | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 8.35 | pKi | 4.46 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Neuropharmacology (2004) 46: 457-67 [PMID:14975669]; J Med Chem (2004) 47: 4570-87 [PMID:15317467] |
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells | B | 5.76 | pIC50 | 1740 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells | B | 4.93 | pIC50 | 11700 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells | B | 5.69 | pIC50 | 2060 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 6.18 | pKi | 664 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
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]
