sergliflozin [Ligand Id: 4587] 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: CHEMBL450044 (GW-869682X, GW869682X, GW-869683X, Sergliflozin, Sergliflozin a, Sergliflozin etabonate) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| Low affinity sodium-glucose cotransporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91] | ||||||||
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem (2011) 19: 5334-5341 [PMID:21873071] |
| Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
| GtoPdb | - | - | 5.1 | pKi | 7943 | nM | Ki | J Pharmacol Exp Ther (2007) 320: 323-30 [PMID:17050778] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem (2011) 19: 5334-5341 [PMID:21873071] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | 158 | nM | Ki | J Pharmacol Exp Ther (2007) 320: 323-30 [PMID:17050778] |
| ChEMBL | Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255] |
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]
