GS39783 [Ligand Id: 5446] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL392394 (GS-39783)
1 CHEMBL392394_lig_chart_1 GABA-B receptor Human
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  • GABAB1/GABA-B receptor 1 in Human [ChEMBL: CHEMBL2064] [GtoPdb: 240] [UniProtKB: Q9UBS5]
  • This target only has 0 pki data point
2 CHEMBL392394_lig_chart_2 GABA-B receptor 1 Human
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  • GABAB receptor in Human [GtoPdb: 242]
  • This target only has 0 pki data point
3 CHEMBL392394_lig_chart_3 GABAB receptor Human
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  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
  • This target only has 0 pki data point
4 CHEMBL392394_lig_chart_4 mGlu5 receptor Rat
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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: 241240] [UniProtKB: O75899Q9UBS5]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]