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Assay Detail

CHEMBL965254

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Reduction of recombinant ECE2 activity measured by McaBk2 fluorescent substrate hydrolysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Endothelin-converting enzyme 2 (CHEMBL5890)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Homology modeling and site-directed mutagenesis to identify selective inhibitors of endothelin-converting enzyme-2.
Gagnidze K, Sachchidanand, Rozenfeld R, Mezei M, Zhou MM, Devi LA.
J Med Chem (2008) 51 : 3378 -3387
PubMed 18507370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.94 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487942 1 5.33
CHEMBL487941 1 5.23
CHEMBL127545 1 5.19
CHEMBL488139 1 4.48
CHEMBL488140 1 4.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487942 IC50 = 4630.0 nM 5.33
CHEMBL487941 IC50 = 5830.0 nM 5.23
CHEMBL127545 IC50 = 6420.0 nM 5.19
CHEMBL488139 IC50 = 32900.0 nM 4.48
CHEMBL488140 IC50 = 35700.0 nM 4.45