NNC-711 [Ligand Id: 4669] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL473104
  • GAT1 in Human [GtoPdb: 929] [UniProtKB: P30531]
  • GAT1/GABA transporter 1 in Mouse [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
  • GAT1/GABA transporter 1 in Rat [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
  • This target only has 0 pki data point
  • 0
1 CHEMBL473104_lig_chart_1 GAT1 HumanMouseRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GAT1 in Human [GtoPdb: 929] [UniProtKB: P30531]
GtoPdb - - 7.4 pIC50 40 nM IC50 Eur J Pharmacol (1994) 269: 219-24 [PMID:7851497]
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as reduction in NO711 binding at incubated for 4 hrs in presence of NO711 by LC-ESI-MS/MS analysis relative to control B 7.58 pKd 26.5 nM Kd Bioorg Med Chem (2019) 27: 2753-2763 [PMID:31097402]
ChEMBL Binding affinity to mouse GAT1 expressed in HEK293 cells membranes using LC-ESI-MS/MS analysis by [2H10]NO711 binding inhibition assay B 6.28 pIC50 <=530 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting B 6.74 pIC50 180 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 417-423 [PMID:26706177]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells B 6.83 pIC50 147.91 nM IC50 Eur. J. Med. Chem. (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]
GAT1/GABA transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
ChEMBL Inhibition of GAT-1 in rat brain homogenate assessed as decrease in [3H]GABA uptake preincubated for 8 mins followed by [3H]GABA addition and measured after 8 mins by scintillation counting analysis B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]

ChEMBL data shown on this page come from version 28:

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]