Molecule Details
InChIKeyUXOWGYHJODZGMF-QORCZRPOSA-N
Compound NameAliskiren
Canonical SMILESCOCCCOc1cc(C[C@@H](C[C@H](N)[C@@H](O)C[C@H](C(=O)NCC(C)(C)C(N)=O)C(C)C)C(C)C)ccc1OC
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL8.17
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB09026
Drug NameAliskiren
CAS Number173334-57-1
Groups approved investigational
ATC Codes C09XA54 C09XA53 C09DX02 C09XA02 C09XA52
DescriptionAliskiren is the first drug in the renin inhibitor drug class and is used for the treatment of hypertension.[A203624] It was developed by Speedel and Novartis and initially approved by the FDA in early 2007.[L14018] Aliskiren has been proven to efficacious in reducing blood pressure when used alone ...

Categories: Acids, Acyclic Agents Acting on the Renin-Angiotensin System Agents causing hyperkalemia Antihypertensive Agents Antihypertensive Agents Indicated for Hypertension Benzene Derivatives Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Substrates Dicarboxylic Acids Enzyme Inhibitors Ethers Hypotensive Agents Methyl Ethers P-glycoprotein substrates Protease Inhibitors Renin Inhibitors
Cross-references: BindingDB: 17950 ChEBI: 601027 CHEMBL1639 ChemSpider: 4591452 Drugs Product Database (DPD): 20175 D03208 PDB: C41 PharmGKB: PA143487910 PubChem:5493444 PubChem:310264980 RxCUI: 325646 Wikipedia: Aliskiren ZINC: ZINC000004393164
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P00797 REN Homo sapiens Human PF07966 PF00026 9.2 IC50 ChEMBL;BindingDB
Q9YQ12 protease Human immunodeficiency virus type 1 Pathogen PF00077 7.1 Ki ChEMBL
DrugBank Target Actions (3)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P00797 REN Renin inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters