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ENaCαβγ

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Target not currently curated in GtoImmuPdb

Target id: 742

Nomenclature: ENaCαβγ

Family: Epithelial sodium channel (ENaC)

Contents:

Quaternary Structure: Subunits
ENaC α
ENaC β
ENaC γ
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of ENaC
PDB Id:  6BQN
Resolution:  3.9Å
Species:  Human
References:  5
Natural/Endogenous Ligands Click here for help
sodium

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Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
S3969 Small molecule or natural product Hs - 5.9 pEC50 - no 4
⤷ pEC50 5.9 (EC50 1.2x10-6 M) [4]
Not voltage dependent
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
BI1265162 Small molecule or natural product Mm Inhibition 8.5 pIC50 - no 2
⤷ pIC50 8.5 (IC50 3x10-9 M) [2]
Not voltage dependent
Description: Inhibition of ENac current in mouse kidney M-l cells in the Ussing chamber assay.
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
P552-02 Small molecule or natural product Hs - no 8.1 pIC50 - no
⤷ pIC50 8.1 (IC50 7.6x10-9 M)
Not voltage dependent
benzamil Small molecule or natural product Click here for species-specific activity table Hs - no ~8.0 pIC50 - no
⤷ pIC50 ~8.0 (IC50 ~1x10-8 M)
Not voltage dependent
amiloride Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs - no 6.7 – 7.0 pIC50 - no
⤷ pIC50 6.7 – 7.0 (IC50 2x10-7 – 1x10-7 M)
Not voltage dependent
triamterene Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs - no ~5.3 pIC50 - no 1,3
⤷ pIC50 ~5.3 (IC50 ~5x10-6 M) [1,3]
Not voltage dependent

References

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1. Canessa CM, Schild L, Buell G, Thorens B, Gautschi I, Horisberger JD, Rossier BC. (1994) Amiloride-sensitive epithelial Na+ channel is made of three homologous subunits. Nature, 367 (6462): 463-7. [PMID:8107805]

2. Heckel A, Frattini S, Hamprecht D, Kley J, Wiedenmayer D. (2017) Novel annelated phenoxyacetamides. Patent number: WO2017028927A1. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 20/08/2015. Publication date: 23/02/2017.

3. Kellenberger S, Gautschi I, Schild L. (2003) Mutations in the epithelial Na+ channel ENaC outer pore disrupt amiloride block by increasing its dissociation rate. Mol Pharmacol, 64 (4): 848-56. [PMID:14500741]

4. Lu M, Echeverri F, Kalabat D, Laita B, Dahan DS, Smith RD, Xu H, Staszewski L, Yamamoto J, Ling J et al.. (2008) Small molecule activator of the human epithelial sodium channel. J Biol Chem, 283 (18): 11981-94. [PMID:18326490]

5. Noreng S, Bharadwaj A, Posert R, Yoshioka C, Baconguis I. (2018) Structure of the human epithelial sodium channel by cryo-electron microscopy. Elife, 7. [PMID:30251954]

Contributors

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