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ChEMBL ligand: CHEMBL2179319 (JNJ-42153605) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
GtoPdb | - | - | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2012) 55: 8770-89 [PMID:23072213] |
ChEMBL | Displacement of [3H]8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-phenyl-1-piperidinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine from mGlu2 receptor (unknown origin) | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Binding affinity to human mGlu2R expressed in CHO cells by radioligand binding assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2012) 55: 8770-8789 [PMID:23072213] |
ChEMBL | Positive allosteric modulation at human mGlu2 receptor W773A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Positive allosteric modulation at human mGlu2 receptor F643A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 6.41 | pEC50 | 385 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Agonist activity at human mGlu2R expressed in CHO cells | F | 6.57 | pEC50 | 270 | nM | EC50 | J Med Chem (2012) 55: 8770-8789 [PMID:23072213] |
ChEMBL | Positive allosteric modulation at wild type human mGlu2 receptor L732A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect preincubated for 30 mins prior to glutamate challenge measured after 30 mins by [35S]GTP-gammaS binding assay | B | 7.33 | pEC50 | 46.4 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Positive allosteric modulation at human mGlu2 receptor N735D mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Positive allosteric modulation at human mGlu2 receptor F776A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 7.63 | pEC50 | 23.6 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
ChEMBL | Positive allosteric modulator activity at human mGlu2R expressed in CHO cells incubated for 30 mins by [35S]GTPgammaS binding assay | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2012) 55: 8770-8789 [PMID:23072213] |
GtoPdb | - | - | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2012) 55: 8770-89 [PMID:23072213] |
ChEMBL | Positive allosteric modulation of wild-type human mGlu2 receptor expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | B | 8.32 | pEC50 | 4.8 | nM | EC50 | J Med Chem (2016) 59: 8495-8507 [PMID:27579727] |
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]