Compound Detail
CHEMBL1200692
OLMESARTAN MEDOXOMIL 💊 Approved Drug
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💊 Approved Drug
CCCc1nc(C(C)(C)O)c(C(=O)OCc2oc(=O)oc2C)n1Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1
Basic Information
| ChEMBL ID | CHEMBL1200692 |
| Name | OLMESARTAN MEDOXOMIL |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UQGKUQLKSCSZGY-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
| Active Moiety | CHEMBL1516 |
5
Targets
7
Activities
2
Assay Types
17
PK Parameters
20
Publications
9
Known Names
12
Indications
1
Mechanisms
Molecular Properties
558.6
MW (Da)
4.17
ALogP
11
HBA
2
HBD
162.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2002 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Type-1 angiotensin II receptor antagonist | ANTAGONIST | Type-1 angiotensin II receptor | ✓ | ✓ |
Indications
Cardiovascular Diseases Diabetes Mellitus Heart Failure Hypertension Myocardial Infarction Stroke Atherosclerosis Diabetic Nephropathies Essential Hypertension Kidney Diseases Proteinuria Glomerulonephritis
ATC Classification
C09CA08
olmesartan medoxomil
Level 1: CARDIOVASCULAR SYSTEM
Level 2: AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
Drug Warnings
Black Box Warning
teratogenicity
Black Box Warning
cardiotoxicity
Activity Summary
IC50 5 meas. best 6.01
Ki 2 meas. best 6.27
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | Ki | 6.27 | 6.27 | 540.0 | 1 |
| Solute carrier organic anion transporter family member 1B3 CHEMBL1743121 | Ki | 6.12 | 6.12 | 750.0 | 1 |
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | IC50 | 6.01 | 6.01 | 977.2 | 1 |
| Solute carrier organic anion transporter family member 1B3 CHEMBL1743121 | IC50 | 6.01 | 6.01 | 977.2 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 5.7 | 5.7 | 2000.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 5.33 | 5.33 | 4730.0 | 1 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.54 | 4.54 | 28500.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 569.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3385.9 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 501.9 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 5160.35 | ng.hr.mL-1 | Homo sapiens |
| Cmax | 223.77 | nM | Rattus norvegicus |
| Cmax | 1595.42 | nM | Rattus norvegicus |
| Cmax | 274.97 | nM | Rattus norvegicus |
| F | 25.0 | % | Homo sapiens |
| T1/2 | 16.67 | hr | - |
| T1/2 | 0.01593 | hr | Rattus norvegicus |
| T1/2 | 0.0825 | hr | Rattus norvegicus |
| T1/2 | 0.0825 | hr | Rattus norvegicus |
| T1/2 | 0.01593 | hr | Rattus norvegicus |
| T1/2 | 16.67 | hr | - |
| Tmax | 0.008333 | hr | Rattus norvegicus |
| Tmax | 2.9 | hr | Rattus norvegicus |
| Tmax | 1.0 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine