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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 |
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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]