biphenylindanone A [Ligand Id: 3954] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL593013 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Binding affinity to human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes by scintillation proximity assay | B | 6.72 | pKd | 190 | nM | Kd | J Med Chem (2017) 60: 6704-6720 [PMID:28704052] |
| ChEMBL | Displacement of [3H]-JNJ46281222 from human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes after 60 mins by liquid scintillation counting method | B | 7.22 | pKi | 60.26 | nM | Ki | J Med Chem (2017) 60: 6704-6720 [PMID:28704052] |
| GtoPdb | - | - | 7 | pEC50 | 111 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4354-8 [PMID:16046122] |
| ChEMBL | Positive allosteric modulation of human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes assessed as increase in glutamate-induced [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 30 mins by Topcount scintillation counting method | F | 7.03 | pEC50 | 93.33 | nM | EC50 | J Med Chem (2017) 60: 6704-6720 [PMID:28704052] |
| ChEMBL | Allosteric modulation of human mGluR2 expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.56 | pEC50 | 27.54 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 175-179 [PMID:19932615] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| ChEMBL | Positive allosteric modulation of rat mGluR2 receptor expressed in HEK293A cells by calcium mobilization assay | F | 6.36 | pEC50 | 441 | nM | EC50 | J Med Chem (2014) 57: 4154-4172 [PMID:24735492] |
| ChEMBL | Positive allosteric modulation of rat mGluR2 expressed in HEK-293 cells assessed as thallium flux through GIRK channels | B | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2011) 54: 342-353 [PMID:21155570] |
| ChEMBL | Positive allosteric modulation activity at rat mGlu2R expressed in HEK293 cells co-expressing GIRK channels by thallium flux assay | B | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2012) 55: 9434-9445 [PMID:23009245] |
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]
