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 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]
