Compound Detail
CHEMBL472
GLYBURIDE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL472 |
| Name | GLYBURIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ZNNLBTZKUZBEKO-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
29
Targets
70
Activities
4
Assay Types
30
PK Parameters
20
Publications
28
Known Names
9
Indications
1
Mechanisms
Molecular Properties
494.0
MW (Da)
3.64
ALogP
5
HBA
3
HBD
113.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
8
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 Diabetes, Gestational Brain Injuries Diabetes Mellitus, Type 1 Stroke Angina, Stable Ischemic Stroke Spinal Cord Injuries
ATC Classification
A10BB01
glibenclamide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 51 meas. best 8.96
Ki 13 meas. best 9.37
EC50 5 meas. best 8.52
Kd 1 meas. best 4.39
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 9.37 | 9.26 | 0.4 | 3 |
| Unchecked CHEMBL612545 | IC50 | 8.96 | 6.8029 | 1.1 | 7 |
| Rattus norvegicus CHEMBL376 | IC50 | 8.8 | 8.8 | 1.6 | 1 |
| Unchecked CHEMBL612545 | EC50 | 8.52 | 7.4 | 3.0 | 3 |
| Sulfonylurea receptor 1, Kir6.2 CHEMBL2096972 | IC50 | 8.37 | 8.37 | 4.3 | 1 |
| Cavia porcellus CHEMBL369 | IC50 | 8.1 | 8.1 | 8.0 | 1 |
| Liver CHEMBL613642 | IC50 | 7.85 | 7.85 | 14.2 | 1 |
| Sulfonylurea receptor 2, Kir6.2 CHEMBL2095198 | Ki | 6.89 | 6.89 | 130.0 | 1 |
| Sulfonylurea receptor 2, Kir6.2 CHEMBL2095198 | IC50 | 6.66 | 6.66 | 220.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | Ki | 6.18 | 6.18 | 660.0 | 1 |
| T-cell line CHEMBL614685 | IC50 | 6.0 | 6.0 | 1000.0 | 1 |
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | IC50 | 5.85 | 5.3967 | 1400.0 | 3 |
| Bile salt export pump CHEMBL6020 | IC50 | 5.82 | 5.378 | 1500.0 | 5 |
| Solute carrier family 22 member 6 CHEMBL1777665 | Ki | 5.8 | 5.8 | 1600.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 5.79 | 5.79 | 1602.0 | 1 |
| CDGSH iron-sulfur domain-containing protein 1 CHEMBL1795168 | Ki | 5.78 | 5.78 | 1671.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | EC50 | 5.64 | 5.64 | 2300.0 | 1 |
| Bile salt export pump CHEMBL2073674 | IC50 | 5.55 | 5.14 | 2800.0 | 3 |
| Mesenchymal stem cells CHEMBL5058627 | EC50 | 5.55 | 5.55 | 2800.0 | 1 |
| Bile salt export pump CHEMBL2073674 | Ki | 5.21 | 5.21 | 6100.0 | 1 |
| Solute carrier family 15 member 2 CHEMBL3325 | Ki | 5.11 | 5.11 | 7800.0 | 1 |
| Leishmania donovani CHEMBL367 | IC50 | 5.01 | 5.01 | 9800.0 | 1 |
| NACHT, LRR and PYD domains-containing protein 3 CHEMBL1741208 | IC50 | 5.0 | 4.96 | 10000.0 | 2 |
| NACHT, LRR and PYD domains-containing protein 3 CHEMBL3779755 | IC50 | 5.0 | 5.0 | 10000.0 | 2 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.98 | 4.98 | 10500.0 | 1 |
| Solute carrier family 22 member 7 CHEMBL2073671 | Ki | 4.91 | 4.91 | 12300.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 4.9 | 4.66 | 12589.2 | 2 |
| Cystic fibrosis transmembrane conductance regulator CHEMBL4051 | IC50 | 4.82 | 4.82 | 15000.0 | 1 |
| Solute carrier family 15 member 1 CHEMBL2073691 | Ki | 4.6 | 4.6 | 25000.0 | 1 |
| Bile salt export pump CHEMBL6020 | Ki | 4.56 | 4.56 | 27500.0 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 4.48 | 4.48 | 33000.0 | 1 |
| CDGSH iron-sulfur domain-containing protein 1 CHEMBL1795168 | IC50 | 4.41 | 4.41 | 39100.0 | 1 |
| Urokinase plasminogen activator surface receptor CHEMBL4883 | Kd | 4.39 | 4.39 | 40400.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 4.13 | 4.13 | 74000.0 | 4 |
| Trypanosoma brucei rhodesiense CHEMBL612348 | IC50 | 4.06 | 4.06 | 87650.0 | 1 |
| Trypanosoma cruzi CHEMBL368 | IC50 | 4.03 | 4.03 | 93930.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 33113.0 | mg/dl | Rattus norvegicus |
| AUC | 2610.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 15230.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3000.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 2350.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 13270.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 2380.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 306.67 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 916.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 356.67 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 1327.4 | ng.hr.mL-1 | Homo sapiens |
| CL | 0.82 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.82 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.82 | mL.min-1.kg-1 | Homo sapiens |
| CL | 14.45 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 22.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 347.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 6.54 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 10.1 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 0.205 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 0.052 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 0.176 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 1.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 69.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.2 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 5.8 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 1.2 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 215.0 | nM | - |
| Cmax | 708.49 | nM | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine