Compound Detail
CHEMBL1073
GLIPIZIDE 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1073 |
| Name | GLIPIZIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ZJJXGWJIGJFDTL-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
4
Activities
2
Assay Types
18
PK Parameters
20
Publications
14
Known Names
5
Indications
1
Mechanisms
Molecular Properties
445.6
MW (Da)
2.08
ALogP
6
HBA
3
HBD
130.2
PSA (Ų)
0.60
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1984 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 blocker | BLOCKER | Sulfonylurea receptor 1, Kir6.2 | ✓ | ✓ |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 2 Atherosclerosis Renal Insufficiency, Chronic Pancreatic Neoplasms
ATC Classification
A10BB07
glipizide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 2 meas. best 6.4
Ki 2 meas. best 8.09
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 8.09 | 7.72 | 8.2 | 2 |
| Unchecked CHEMBL612545 | IC50 | 6.4 | 6.4 | 398.0 | 1 |
| Cytochrome P450 3A4 CHEMBL340 | IC50 | 5.13 | 5.13 | 7447.3 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 0.96 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.56 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.56 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.56 | mL.min-1.kg-1 | Homo sapiens |
| CL | 4.27 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 4.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.24 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 0.53 | mL.min-1.kg-1 | Homo sapiens |
| F | 80.0 | % | Homo sapiens |
| F | 95.0 | % | Homo sapiens |
| F | 95.0 | % | Homo sapiens |
| Fu | 0.02 | - | Homo sapiens |
| Fu | 0.02 | - | Homo sapiens |
| Fu | 0.000138 | - | Macaca fascicularis |
| Fu | 0.000402 | - | Homo sapiens |
| MRT | 4.8 | hr | Homo sapiens |
| T1/2 | 3.3 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | Ki | = | 8.2 | nM | 8.09 | Inhibition of [125I]-I binding to ATP-inhibited Potassium channel receptor of Ra... | 2124268 |
| Unchecked | Ki | = | 45.0 | nM | 7.35 | DRUGMATRIX: Potassium Channel [KATP] radioligand binding (ligand: [3H] Glyburide... | - |
| Unchecked | IC50 | = | 398.0 | nM | 6.4 | DRUGMATRIX: Potassium Channel [KATP] radioligand binding (ligand: [3H] Glyburide... | - |
| Cytochrome P450 3A4 | IC50 | = | 7447.32 | nM | 5.13 | Inhibition of CYP3A4 | 19128860 |
Literature References
Data from ChEMBL 36 via Core Engine