Molecule Details
InChIKeyMCIACXAZCBVDEE-CUUWFGFTSA-N
Compound NameErtugliflozin
Canonical SMILESCCOc1ccc(Cc2cc([C@]34OC[C@](CO)(O3)[C@@H](O)[C@H](O)[C@H]4O)ccc2Cl)cc1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL8.18
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB11827
Drug NameErtugliflozin
CAS Number1210344-57-2
Groups approved investigational
ATC Codes A10BD23 A10BK04 A10BD24
DescriptionErtugliflozin is a sodium-dependent glucose cotransporter-2 (SGLT2) inhibitor used to treat type II diabetes mellitus. It works to block glucose reabsorption from the glomerulus.[A31581] Ertugliflozin was first approved by the FDA in December 2017.[A261951, L1132] It was also approved by the Europea...

Categories: Alimentary Tract and Metabolism BCRP/ABCG2 Substrates Blood Glucose Lowering Agents Diuretics Drugs Used in Diabetes P-glycoprotein substrates Sodium-Glucose Transporter 2 Inhibitors Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors UGT1A1 Inhibitors UGT1A4 Inhibitors UGT1A9 Substrates UGT2B7 substrates
Cross-references: BindingDB: 50342885 ChEBI: 188719 CHEMBL1770248 ChemSpider: 26340533 Drugs Product Database (DPD): 22949 PharmGKB: PA166269521 PubChem:44814423 PubChem:347828173 RxCUI: 1992672 Wikipedia: Ertugliflozin ZINC: ZINC000068197809
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P31639 SLC5A2 Homo sapiens Human PF00474 9.1 IC50 ChEMBL;BindingDB
Q9NY91 SLC5A4 Homo sapiens Human PF00474 9.1 IC50 BindingDB
P13866 SLC5A1 Homo sapiens Human PF00474 6.4 IC50 ChEMBL;BindingDB
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P02768 ALB Albumin binder carriers
P22309 UGT1A1 UDP-glucuronosyltransferase 1A1 inhibitor enzymes
P22310 P22310 UDP-glucuronosyltransferase 1A4 inhibitor enzymes
O60656 O60656 UDP-glucuronosyltransferase 1A9 substrate enzymes
P16662 UGT2B7 UDP-glucuronosyltransferase 2B7 substrate enzymes
P31639 SLC5A2 Sodium/glucose cotransporter 2 inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters