SKF89976A [Ligand Id: 4705] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38686 (SKF-89976)
  • GAT1/GABA transporter 1 in Human [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
  • GAT1/GABA transporter 1 in Mouse [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
  • This target only has 1 pki data point
  • 6.73
1 CHEMBL38686_lig_chart_1 GABA transporter 1 HumanMouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GAT1/GABA transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
ChEMBL Binding affinity to GAT1 B 6.7 pIC50 200 nM IC50 Eur. J. Med. Chem. (2010) 45: 2453-2466 [PMID:20219271]
ChEMBL Compound was tested for its ability to inhibit uptake of [3H]- GABA by cloned human GAT-1 transporter F 6.89 pIC50 130 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 1535-1540
ChEMBL Inhibition of human GAT1 expressed in COS cells assessed as decrease in [3H]GABA uptake after 10 mins by scintillation counting analysis B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]
GtoPdb - - 6.9 pIC50 130 nM IC50 Bioorg Med Chem Lett (1996) 6: 1535 -1540
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL Displacement of NO 711 from mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS-based MS binding assay B 6.73 pKi 186.21 nM Ki Bioorg. Med. Chem. (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells B 6.16 pIC50 691.83 nM IC50 Eur. J. Med. Chem. (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL Inhibition of GABA uptake at murine GAT-1 expressed in HEK293 cells B 6.16 pIC50 691.83 nM IC50 Eur. J. Med. Chem. (2013) 65: 487-499 [PMID:23770450]
ChEMBL Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis B 6.89 pIC50 130 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 6.9 pIC50 125.89 nM IC50 J. Med. Chem. (2013) 56: 1323-1340 [PMID:23336362]

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]