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

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ChEMBL ligand: CHEMBL38686 (SKF-89976)
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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 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]