Compound Detail
CHEMBL539423
SPARSENTAN 💊 Approved Drug
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💊 Approved Drug
CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2noc(C)c2C)c(COCC)c1
Basic Information
| ChEMBL ID | CHEMBL539423 |
| Name | SPARSENTAN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WRFHGDPIDHPWIQ-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
6
Known Names
3
Indications
2
Mechanisms
Molecular Properties
592.8
MW (Da)
6.54
ALogP
7
HBA
1
HBD
114.1
PSA (Ų)
0.26
QED
2
Ro5 Violations
12
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2023 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Endothelin receptor ET-A antagonist | ANTAGONIST | Endothelin-1 receptor | ✓ | ✓ |
| Type-1 angiotensin II receptor antagonist | ANTAGONIST | Type-1 angiotensin II receptor | ✓ | ✓ |
Indications
Glomerulonephritis, IGA Glomerulosclerosis, Focal Segmental Hypertension
ATC Classification
C09XX01
sparsentan
Level 1: CARDIOVASCULAR SYSTEM
Level 2: AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
Drug Warnings
Black Box Warning
teratogenicity
Black Box Warning
hepatotoxicity
Activity Summary
Ki 4 meas. best 9.1
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Type-1 angiotensin II receptor CHEMBL227 | Ki | 9.1 | 9.1 | 0.8 | 2 |
| Endothelin-1 receptor CHEMBL252 | Ki | 8.03 | 8.03 | 9.3 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Type-1 angiotensin II receptor | Ki | = | 0.8 | nM | 9.1 | Inhibitory concentration against angiotensin II receptor, type 1 | 16220969 |
| Type-1 angiotensin II receptor | Ki | = | 0.8 | nM | 9.1 | Binding affinity to AT1 receptor | 22931505 |
| Endothelin-1 receptor | Ki | = | 9.3 | nM | 8.03 | Inhibitory concentration against endothelin receptor type A | 16220969 |
| Endothelin-1 receptor | Ki | = | 9.3 | nM | 8.03 | Binding affinity to ETA receptor | 22931505 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 15634011 | 10.1021/jm049548x | Angiotensin II receptor (AT-1) type-1 | 1 |
| 15634011 | 10.1021/jm049548x | Endothelin-1 receptor | 1 |
| 16220969 | 10.1021/jm058225d | Endothelin-1 receptor | 1 |
| 16220969 | 10.1021/jm058225d | Type-1 angiotensin II receptor | 1 |
| 22931505 | 10.1021/jm300682j | Endothelin-1 receptor | 1 |
| 22931505 | 10.1021/jm300682j | Type-1 angiotensin II receptor | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine