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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
