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 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]
