Molecule Details
InChIKeyZNNLBTZKUZBEKO-UHFFFAOYSA-N
Compound NameGlibenclamide
Canonical SMILESCOc1ccc(Cl)cc1C(=O)NCCc1ccc(S(=O)(=O)NC(=O)NC2CCCCC2)cc1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)5
Pfam Stratification Cross-Family
Avg pChEMBL7.25
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB01016
Drug NameGlyburide
CAS Number10238-21-8
Groups approved investigational
ATC Codes A10BB01
DescriptionGlyburide is a second generation sulfonylurea used to treat patients with diabetes mellitus type II.[L8123] It is typically given to patients who cannot be managed with the standard first line therapy, [metformin].[L8123] Glyburide stimulates insulin secretion through the closure of ATP-sensitive po...

Categories: Alimentary Tract and Metabolism Amides BCRP/ABCG2 Substrates BSEP/ABCB11 Inhibitors BSEP/ABCB11 Substrates Blood Glucose Lowering Agents Cytochrome P-450 CYP2C19 Substrates Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (strength unknown) Cytochrome P-450 CYP2C9 Substrates Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A5 Substrates Cytochrome P-450 CYP3A7 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Drugs Used in Diabetes Drugs causing inadvertant photosensitivity Hypoglycemia-Associated Agents Insulin Secretagogues OAT1/SLC22A6 inhibitors OATP2B1/SLCO2B1 substrates Oral Hypoglycemics P-glycoprotein inhibitors Photosensitizing Agents Sulfones Sulfonylureas Sulfur Compounds
Cross-references: BindingDB: 50012957 ChEBI: 5441 CHEMBL472 ChemSpider: 3368 Drugs Product Database (DPD): 4007 Guide to Pharmacology: 2414 IUPHAR: 2414 C07022 D00336 PDB: GBM PharmGKB: PA449782 PubChem:3488 PubChem:46509154 RxCUI: 4815 Therapeutic Targets Database: DAP000037 Wikipedia: Glibenclamide ZINC: ZINC000000537805
Target Activities (5)
Target Gene Organism Category Pfam pChEMBL Type Source
Q09428 ABCC8 Homo sapiens Human PF00664 PF00005 8.4 IC50 ChEMBL
Q15526 SURF1 Homo sapiens Human PF02104 8.1 IC50 BindingDB
Q14654 KCNJ11 Homo sapiens Human PF01007 PF17655 6.9 IC50 ChEMBL;BindingDB
O60706 ABCC9 Homo sapiens Human PF00664 PF00005 6.8 IC50 ChEMBL
P37231 PPARG Homo sapiens Human PF00104 PF12577 PF00105 6.2 Ki ChEMBL;BindingDB
DrugBank Target Actions (30)
Target Gene Target Name Action Type
P02768 ALB Albumin binder carriers
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P11712 CYP2C9 Cytochrome P450 2C9 substrate enzymes
P20815 CYP3A5 Cytochrome P450 3A5 substrate enzymes
P24462 CYP3A7 Cytochrome P450 3A7 substrate enzymes
P33261 CYP2C19 Cytochrome P450 2C19 substrate enzymes
P13569 CFTR Cystic fibrosis transmembrane conductance regulator antagonist targets
Q09428 ABCC8 Sulfonylurea receptor 1, Kir6.2 blocker targets
O95342 ABCB11 Bile salt export pump inhibitor targets
O95477 O95477 Phospholipid-transporting ATPase ABCA1 inhibitor targets
P50416 CPT1A Carnitine O-palmitoyltransferase 1, liver isoform inhibitor targets
Q14654 KCNJ11 Mitochondrial ATP-sensitive potassium channel inhibitor targets
Q8TD43 Q8TD43 Transient receptor potential cation channel subfamily M member 4 inhibitor targets
O60706 ABCC9 ATP-binding cassette sub-family C member 9 modulator targets
Q09428 ABCC8 ATP-binding cassette sub-family C member 8 modulator targets
O15438 ABCC3 ATP-binding cassette sub-family C member 3 inhibitor transporters
O95342 ABCB11 Bile salt export pump inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
P33527 ABCC1 Multidrug resistance-associated protein 1 inhibitor transporters
P46059 SLC15A1 Solute carrier family 15 member 1 inhibitor transporters
P46721 P46721 Solute carrier organic anion transporter family member 1A2 inhibitor transporters
Q16348 Q16348 Solute carrier family 15 member 2 inhibitor transporters
Q4U2R8 SLC22A6 Solute carrier family 22 member 6 inhibitor transporters
Q92887 ABCC2 ATP-binding cassette sub-family C member 2 inhibitor transporters
Q9Y694 Q9Y694 Solute carrier family 22 member 7 inhibitor transporters
O94956 SLCO2B1 Solute carrier organic anion transporter family member 2B1 substrate transporters
O95342 ABCB11 Bile salt export pump substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters