Compound Detail
CHEMBL1481
GLIMEPIRIDE 💊 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
CCC1=C(C)CN(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)N[C@H]3CC[C@H](C)CC3)cc2)C1=O
Basic Information
| ChEMBL ID | CHEMBL1481 |
| Name | GLIMEPIRIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WIGIZIANZCJQQY-RUCARUNLSA-N |
| Therapeutic | ✓ Yes |
6
Targets
11
Activities
3
Assay Types
30
PK Parameters
20
Publications
9
Known Names
7
Indications
1
Mechanisms
Molecular Properties
490.6
MW (Da)
3.07
ALogP
5
HBA
3
HBD
124.7
PSA (Ų)
0.54
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1995 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
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 Diabetes Mellitus, Type 2 Atherosclerosis Coronary Disease Hypercholesterolemia Hypertension
ATC Classification
A10BB12
glimepiride
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 9 meas. best 8.39
EC50 1 meas. best 6.1
Ki 1 meas. best 7.96
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | IC50 | 8.39 | 7.695 | 4.1 | 2 |
| Unchecked CHEMBL612545 | Ki | 7.96 | 7.96 | 11.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 6.1 | 6.1 | 790.0 | 1 |
| Aldo-keto reductase family 1 member C3 CHEMBL4681 | IC50 | 6.07 | 6.07 | 850.0 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 5.19 | 5.19 | 6390.0 | 1 |
| Aldo-keto reductase family 1 member C1 CHEMBL5905 | IC50 | 5.16 | 5.16 | 6860.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.8 | 4.69 | 15700.0 | 3 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.19 | 4.19 | 64000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 338.8 | ng.hr.mL-1 | Homo sapiens |
| AUC | 315.2 | ng.hr.mL-1 | Homo sapiens |
| AUC | 1665.69 | ng.hr.mL-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.5 | mL.min-1.kg-1 | Homo sapiens |
| CL | 23.2 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 5.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.62 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 6.17 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 0.69 | mL.min-1.kg-1 | Homo sapiens |
| CL | 47.8 | mL/min | Homo sapiens |
| CL/F | 52.1 | mL/min | Homo sapiens |
| CL/F | 48.5 | mL/min | Homo sapiens |
| CL/F | 52.7 | mL/min | Homo sapiens |
| Cmax | 209.93 | nM | Homo sapiens |
| Cmax | 208.71 | nM | Homo sapiens |
| Cmax | 210.34 | nM | Homo sapiens |
| Cmax | 717.44 | nM | Homo sapiens |
| Cmax | 627.76 | nM | Homo sapiens |
| Cmax | 360.76 | nM | Homo sapiens |
| Cmax | 1123.05 | nM | Homo sapiens |
| Cmax | 1204.57 | nM | Homo sapiens |
| Cmax | 1178.08 | nM | Homo sapiens |
| Cmax | 629.8 | nM | Homo sapiens |
| Cmax | 1123.0 | nM | Homo sapiens |
| F | 100.0 | % | Homo sapiens |
| Fu | 0.005 | - | Homo sapiens |
| Fu | 0.005 | - | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine