NNC-711 [Ligand Id: 4669] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL473104 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| 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 mouse GAT1 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | B | 6.83 | pIC50 | 147.91 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| 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 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]
