Molecule Details
| InChIKey | ZNNLBTZKUZBEKO-UHFFFAOYSA-N |
|---|---|
| Compound Name | Glibenclamide |
| Canonical SMILES | COc1ccc(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 pChEMBL | 7.25 |
| Source | BindingDB;ChEMBL |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB01016 |
|---|---|
| Drug Name | Glyburide |
| CAS Number | 10238-21-8 |
| Groups | approved investigational |
| ATC Codes | A10BB01 |
| Description | Glyburide 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 |