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ChEMBL ligand: CHEMBL40086 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Affinity value against N-methyl-D-aspartate (NMDA) receptor using [3H]-CGS- 19755 in glutamate radioligand binding assay. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
ChEMBL | Affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA in selective radioligand binding assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
ChEMBL | Affinity value against Ionotropic glutamate receptor kainate using [3H]-kainic acid in selective radioligand binding assay. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
ChEMBL | Agonist potency against cloned human metabotropic glutamate receptor 1 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 1 | F | 4 | pEC50 | 100000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
GtoPdb | - | - | 5 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2). | F | 6.35 | pKi | 450 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
ChEMBL | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 2 | F | 6.32 | pEC50 | 480 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1919-1924 [PMID:11459661] |
ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 2 | F | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing mGluR2 receptor | F | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
GtoPdb | - | - | 5.3 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 6.39 | pKi | 410 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor | F | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
ChEMBL | Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3 | F | 5.77 | pEC50 | 1700 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1919-1924 [PMID:11459661] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
ChEMBL | Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2005) 48: 2534-2547 [PMID:15801843] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
ChEMBL | Agonist potency against cloned metabotropic glutamate receptor 5 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
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]