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ChEMBL ligand: CHEMBL277475 |
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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 | Displacement of [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat brain membrane | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
ChEMBL | Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) | F | 5.28 | pKi | 5200 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | F | 5.28 | pEC50 | 5200 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
GtoPdb | - | - | 5.3 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390] |
ChEMBL | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | B | 5.33 | pEC50 | 4700 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1447-1450 [PMID:10888329] |
ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | F | 5.49 | pEC50 | 3200 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
ChEMBL | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.28 | pEC50 | 5200 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6). | F | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
GtoPdb | - | - | 5.3 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
ChEMBL | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.33 | pEC50 | 4700 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
GtoPdb | - | - | 3.7 | pIC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390] |
ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7b | F | 4.32 | pEC50 | 48000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
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 | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
GtoPdb | - | - | 6.7 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390]; Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
ChEMBL | Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.68 | pEC50 | 210 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
ChEMBL data shown on this page come from version 32:
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]