amiloride

Ligand id: 2421

Name: amiloride

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 4
Rotatable bonds 2
Topological polar surface area 159.29
Molecular weight 229.05
XLogP -1.18
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
ENaCαβγ Hs Channel blocker - 6.7 – 7.0 pIC50 -
pIC50 6.7 – 7.0 (IC50 2x10-7 – 1x10-7 M)
ASIC1 Hs Channel blocker - 4.6 – 5.0 pIC50 -
pIC50 5.0 (IC50 1x10-5 M) ASIC1a
pIC50 4.6 – 4.7 (IC50 2.3x10-5 – 2.1x10-5 M) ASIC1b
ASIC2 Hs Channel blocker - 4.6 pIC50 -
pIC50 4.6 (IC50 2.8x10-5 M)
ASIC3 Hs Channel blocker - 4.2 – 4.8 pIC50 -
pIC50 4.2 – 4.8 (IC50 6.3x10-5 – 1.6x10-5 M) transient component only - sustained component enhanced by 200μM amiloride at pH 4
TRPC6 Mm Channel blocker Antagonist 3.9 pIC50 - 2
pIC50 3.9 (IC50 1.29x10-4 M) [2]
Voltage: -60.0 mV
TRPP2 Hs Channel blocker - 3.8 pIC50 -
pIC50 3.8 (IC50 1.43x10-4 M)
TRPA1 Mm Channel blocker Inhibition 3.3 pIC50 - 7
pIC50 3.3 [7]
Voltage: -80.0 mV
TRPC7 Hs Channel blocker - - - -
TRPV2 Hs Channel blocker - - - -
Selectivity at transporters
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
Sodium/hydrogen exchanger 2 Oc Inhibitor Inhibition 6.3 – 7.1 pKi - 4
pKi 6.3 – 7.1 (Ki 5x10-7 – 8x10-8 M) [4]
Sodium/hydrogen exchanger 1 Rn Inhibitor Inhibition 5.8 – 6.0 pKi - 4
pKi 5.8 – 6.0 (Ki 1.6x10-6 – 1x10-6 M) [4]
Sodium/hydrogen exchanger 5 Hs Inhibitor Inhibition 4.7 pKi - 4
pKi 4.7 (Ki 2.1x10-5 M) [4]
Sodium/hydrogen exchanger 3 Rn Inhibitor Inhibition <4.0 pKi - 4
pKi <4.0 (Ki >1x10-4 M) [4]
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