Molecule Details
InChIKeyXSDQTOBWRPYKKA-UHFFFAOYSA-N
Compound NameAmiloride
Canonical SMILESN=C(N)NC(=O)c1nc(Cl)c(N)nc1N
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Cross-Family
Avg pChEMBL6.11
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB00594
Drug NameAmiloride
CAS Number2609-46-3
Groups approved investigational
ATC Codes C03DB01
DescriptionA pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassi...

Categories: Acid Sensing Ion Channel Blockers Agents causing hyperkalemia Cardiovascular Agents Decreased Renal K+ Excretion Diuretics Epithelial Sodium Channel Blockers Hypotensive Agents Increased Diuresis Membrane Transport Modulators Natriuretic Agents OCT2 Inhibitors Potassium-Sparing Diuretics Pyrazines Sodium Channel Blockers
Cross-references: BindingDB: 16173 ChEBI: 2639 CHEMBL945 ChemSpider: 15403 Drugs Product Database (DPD): 20230 Guide to Pharmacology: 2421 IUPHAR: 2421 C06821 D07447 PDB: AMR PharmGKB: PA448368 PubChem:16231 PubChem:46508156 RxCUI: 644 Therapeutic Targets Database: DAP000187 Wikipedia: Amiloride ZINC: ZINC000004340269
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P37088 SCNN1A Homo sapiens Human PF00858 6.1 IC50 ChEMBL;BindingDB
Q14524 SCN5A Homo sapiens Human PF00520 PF24609 PF06512 PF11933 6.1 IC50 BindingDB
DrugBank Target Actions (13)
Target Gene Target Name Action Type
P19801 AOC1 Diamine oxidase [copper-containing] inhibitor enzymes
Q9TRC7 Q9TRC7 Diamine oxidase [copper-containing] inhibitor enzymes
P00749 PLAU Urokinase-type plasminogen activator inhibitor targets
P19634 SLC9A1 Sodium/hydrogen exchanger 1 inhibitor targets
P19801 AOC1 Diamine oxidase [copper-containing] inhibitor targets
P37088 SCNN1A Epithelial sodium channel subunit alpha inhibitor targets
P51168 SCNN1B Epithelial sodium channel subunit beta inhibitor targets
P51170 SCNN1G Epithelial sodium channel subunit gamma inhibitor targets
P51172 P51172 Epithelial sodium channel subunit delta inhibitor targets
P78348 ASIC1 Acid-sensing ion channel 1 inhibitor targets
Q16515 Q16515 Acid-sensing ion channel 2 inhibitor targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
Q9H015 Q9H015 Solute carrier family 22 member 4 inhibitor transporters