ertugliflozin [Ligand Id: 8376] 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: CHEMBL1770248 (Ertugliflozin, Ertugliflozina, Ertugliflozine, MK-8835, Pf-04971729, PF-04971729, PF04971729, PF-04971729-00, Steglatro) |
|---|
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 inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr | B | 9.06 | pIC50 | 0.88 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
| Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
| ChEMBL | Inhibition of human SGLT1 | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr | B | 5.71 | pIC50 | 1960 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
| ChEMBL | Inhibition of human SGLT1 | B | 5.71 | pIC50 | 1960 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 5.71 | pIC50 | 1960 | nM | IC50 | J Med Chem (2011) 54: 2952-60 [PMID:21449606] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 6.41 | pIC50 | 392 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| ChEMBL | Inhibition of human SGLT2 | B | 9.06 | pIC50 | 0.88 | nM | IC50 | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
| ChEMBL | Inhibition of human SGLT2 | B | 9.06 | pIC50 | 0.88 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 9.06 | pIC50 | 0.88 | nM | IC50 | J Med Chem (2011) 54: 2952-60 [PMID:21449606] |
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Medchemcomm (2018) 9: 1273-1281 [PMID:30151080] |
| Sodium/glucose cotransporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4316] [GtoPdb: 916] [UniProtKB: P53792] | ||||||||
| ChEMBL | Inhibition of rat SGLT2 | B | 8.94 | pIC50 | 1.15 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
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]
