Compound Detail
CHEMBL57242
AZILSARTAN 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL57242 |
| Name | AZILSARTAN |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | KGSXMPPBFPAXLY-UHFFFAOYSA-N |
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
18
Publications
2
Known Names
6
Indications
1
Mechanisms
Molecular Properties
456.5
MW (Da)
4.19
ALogP
7
HBA
2
HBD
123.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Type-1 angiotensin II receptor antagonist | ANTAGONIST | Type-1 angiotensin II receptor | ✓ | ✓ |
Indications
Diabetes Mellitus, Type 2 Essential Hypertension Hypertension Severe Acute Respiratory Syndrome Severe Acute Respiratory Syndrome Diabetes Mellitus
Activity Summary
IC50 2 meas. best 6.38
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Type-1 angiotensin II receptor CHEMBL3374 | IC50 | 6.38 | 6.38 | 420.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.38 | 6.38 | 420.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| F | 20.0 | % | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Type-1 angiotensin II receptor | IC50 | = | 420.0 | nM | 6.38 | Displacement of [125 I]-AII (0.2 nM) from bovine adrenal cortical membrane angio... | - |
| Unchecked | IC50 | = | 420.0 | nM | 6.38 | Inhibition of specific binding of [125I]angiotensin II (0.2 nM) to angiotensin I... | 8978851 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.1016/0960-894X(95)00319-O | Rattus norvegicus | 5 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 8978851 | 10.1021/jm960547h | No relevant target | 2 |
| 34413955 | 10.1021/acsmedchemlett.1c00240 | Leukotriene B4 receptor 2 | 1 |
| - | 10.1016/0960-894X(95)00319-O | Type-1 angiotensin II receptor | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| - | 10.1101/2020.04.21.054387 | SARS-CoV-2 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 21071232 | 10.1016/j.bmc.2010.10.043 | Rattus norvegicus | 1 |
| 21071232 | 10.1016/j.bmc.2010.10.043 | Type-1 angiotensin II receptor | 1 |
| 8978851 | 10.1021/jm960547h | ADMET | 1 |
| 8978851 | 10.1021/jm960547h | Rattus norvegicus | 1 |
| 8978851 | 10.1021/jm960547h | Angiotensin II receptor | 1 |
| 8978851 | 10.1021/jm960547h | Unchecked | 1 |
| - | 10.1016/0960-894X(95)00319-O | No relevant target | 1 |
| - | 10.1016/0960-894X(95)00319-O | ADMET | 1 |
Data from ChEMBL 36 via Core Engine