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Endothelin-converting enzyme 1

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Target not currently curated in GtoImmuPdb

Target id: 1615

Nomenclature: Endothelin-converting enzyme 1

Abbreviated Name: ECE1

Family: M13: Neprilysin

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 770 1p36.12 ECE1 endothelin converting enzyme 1
Mouse 1 769 4 D3 Ece1 endothelin converting enzyme 1
Rat 1 762 5q36 Ece1 endothelin converting enzyme 1
Previous and Unofficial Names Click here for help
ECE-1 | ECE
Database Links Click here for help
Specialist databases
MEROPS M13.002 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.24.71
Endogenous substrates (Human)
endothelin-1 (EDN1, P05305), endothelin-2 (EDN2, P20800), endothelin-3 (EDN3, P14138)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 22 [PMID: 19899765] Small molecule or natural product Hs Inhibition 5.9 pKi 2
pKi 5.9 (Ki 1.2x10-6 M) [2]
PD159790 Small molecule or natural product Primary target of this compound Hs Inhibition 5.6 pKi 1
pKi 5.6 (Ki 2.3x10-6 M) [1]
SM19712 Small molecule or natural product Rn Inhibition 7.4 pIC50 4
pIC50 7.4 (IC50 4.2x10-8 M) [4]
KC-12615 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pIC50 3
pIC50 5.8 (IC50 1.5x10-6 M) [3]
daglutril Small molecule or natural product Click here for species-specific activity table Hs Inhibition - -
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Hirschsprung disease, cardiac defects, and autonomic dysfunction
OMIM: 613870
Disease:  Hypertension, essential
Disease Ontology: DOID:10825
OMIM: 145500

References

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1. Ahn K, et al. (1996) Quinazolines as inhibitors of endothelin converting enzyme. Patent number: WO1996019474. Assignee: Warner Lambert. Priority date: 22/12/1994. Publication date: 22/06/1996.

2. Jullien N, Makritis A, Georgiadis D, Beau F, Yiotakis A, Dive V. (2010) Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. J. Med. Chem., 53 (1): 208-20. [PMID:19899765]

3. Seed A, Kuc RE, Maguire JJ, Hillier C, Johnston F, Essers H, de Voogd HJ, McMurray J, Davenport AP. (2012) The dual endothelin converting enzyme/neutral endopeptidase inhibitor SLV-306 (daglutril), inhibits systemic conversion of big endothelin-1 in humans. Life Sci., 91 (13-14): 743-8. [PMID:22480515]

4. Umekawa K, Hasegawa H, Tsutsumi Y, Sato K, Matsumura Y, Ohashi N. (2000) Pharmacological characterization of a novel sulfonylureid-pyrazole derivative, SM-19712, a potent nonpeptidic inhibitor of endothelin converting enzyme. Jpn. J. Pharmacol., 84 (1): 7-15. [PMID:11043447]

How to cite this page

M13: Neprilysin: Endothelin-converting enzyme 1. Last modified on 21/07/2015. Accessed on 20/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1615.