GS39783 [Ligand Id: 5446] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL392394 (GS-39783) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5] | ||||||||
| ChEMBL | Activity at GABAB 1b/2 receptor expressed in CHO-K1 cells assessed as effect on glutamate-induced [35S]GTP-gamma-S binding | F | 6.13 | pEC50 | 741.31 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6206-6211 [PMID:17884493] |
| GABAB1/GABA-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2064] [GtoPdb: 240] [UniProtKB: Q9UBS5] | ||||||||
| ChEMBL | Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone | B | 7.1 | pEC50 | 79.43 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 2239-2258 [PMID:28408223] |
| GABAB receptor in Human [GtoPdb: 242] | ||||||||
| mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
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]
