amiloride
A 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 potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
Ligand Summary
UNII: 7DZO8EB0Z3
PubChem: 16231
Guide to Pharmacology: 2421
ChEMBL: CHEMBL945
DrugCentral: 158
LyCHI: 1DKCKQ65KQGJ
Target Activities
ASIC1
Acid-sensing ion channel 1
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5 | |||||
IC50 | 5 | |||||
SCNN1A
Amiloride-sensitive sodium channel subunit alpha
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.11 | J. Med. Chem., (2006) 49:14:4098 | ||||
IC50 | 6.7 | BLOCKER | ||||
ASIC3
Acid-sensing ion channel 3
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.36 | Bioorg. Med. Chem. Lett., (2009) 19:9:2514 | ||||
IC50 | 5.36 | |||||
ASIC2
Acid-sensing ion channel 2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 4.6 | |||||
SLC9A3
Sodium/hydrogen exchanger 3
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 4 | |||||
SLC9A5
Sodium/hydrogen exchanger 5
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 4.68 | |||||
TRPA1
Transient receptor potential cation channel subfamily A member 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 3.3 | |||||
TRPC6
Short transient receptor potential channel 6
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 3.9 | |||||
PKD2L1
Polycystic kidney disease 2-like 1 protein
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 3.8 | |||||
SCNN1B
Amiloride-sensitive sodium channel subunit beta
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.7 | BLOCKER | ||||
SCNN1G
Amiloride-sensitive sodium channel subunit gamma
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.7 | BLOCKER | ||||