| Compound Information | SONAR Target prediction |
| Name: | GLYBURIDE |
| Unique Identifier: | SPE02300229 |
| MolClass: | Checkout models in ver1.5 and ver1.0 |
| Molecular Formula: | |
| Molecular Weight: | 465.782 g/mol |
| X log p: | 14.163 (online calculus) |
| Lipinksi Failures | 2 |
| TPSA | 85.89 |
| Hydrogen Bond Donor Count: | 0 |
| Hydrogen Bond Acceptors Count: | 8 |
| Rotatable Bond Count: | 11 |
| Canonical Smiles: | COc1ccc(Cl)cc1C(=O)NCCc1ccc(cc1)S(=O)(=O)NC(=O)NC1CCCCC1 |
| Source: | synthetic |
| Therapeutics: | antihyperglycemic |
| Generic_name: | Glyburide |
| Chemical_iupac_name: | 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxy-benzamide |
| Drug_type: | Approved Drug |
| Pharmgkb_id: | PA449782 |
| Kegg_compound_id: | C07022 |
| Drugbank_id: | APRD00233 |
| Melting_point: | 169-170oC |
| H2o_solubility: | 4 mg/L |
| Logp: | 4.85 |
| Cas_registry_number: | 10238-21-8 |
| Drug_category: | Hypoglycemic Agents; Antiarrhythmic Agents; Sulfonylureas; ATC:A10BB |
| Indication: | Indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone. |
| Pharmacology: | Glyburide, a second-generation sulfonylurea antidiabetic agent, appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glyburide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glyburide produces a mild diuresis by enhancement of renal free water clearance. Glyburide is twice as potent as the related second-generation agent glipizide. |
| Mechanism_of_action: | Sulfonylureas such as glyburide likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin. |
| Organisms_affected: | Humans and other mammals |
| Found: 205 nonactive as graph: single | with analogs | 1 2 3 4 5 6 7 8 9 10 Next >> [205] |
| Species: | 4932 |
| Condition: | BCK1 |
| Replicates: | 2 |
| Raw OD Value: r im | 0.8620±0.0211425 |
| Normalized OD Score: sc h | 0.9794±0.0132475 |
| Z-Score: | -0.7131±0.246269 |
| p-Value: | 0.482402 |
| Z-Factor: | -3.47804 |
| Fitness Defect: | 0.729 |
| Bioactivity Statement: | Nonactive |
| ps |
| DBLink | Rows returned: 1 |
| 3488 | 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxy-benzamide |
| internal high similarity DBLink | Rows returned: 2 |
| LOPAC 00193 | 1.0000 |
| RJC 01668 | 1.0000 |
| active | Cluster 5012 | Additional Members: 11 | Rows returned: 1 |
| Prest1231 | 0.48936170212766 |
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