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Assay Detail

CHEMBL679844

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

Binding
In vitro inhibition of Endothelin-converting enzyme 1.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-converting enzyme 1 (CHEMBL4791)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1.
Firooznia F, Gude C, Chan K, Tan J, Fink CA, Savage P, Beil ME, Bruseo CW, Trapani AJ, Jeng AY.
Bioorg Med Chem Lett (2002) 12 : 3059 -3062
PubMed 12372501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.32 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317472 1 8.02
CHEMBL102527 1 8.01
CHEMBL292748 1 7.96
CHEMBL319463 1 7.64
CHEMBL421021 1 7.62
CHEMBL102815 1 7.57
CHEMBL103327 1 7.52
CHEMBL419170 1 7.41
CHEMBL421586 1 7.39
CHEMBL105054 1 7.37
CHEMBL320400 1 7.31
CHEMBL103378 1 7.26
CHEMBL104617 1 7.25
CHEMBL103966 1 7.19
CHEMBL64081 1 7.11
CHEMBL104814 1 7.11
CHEMBL102795 1 7.09
CHEMBL320471 1 7.01
CHEMBL319708 1 6.92
CHEMBL419725 1 6.89
CHEMBL441817 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317472 IC50 = 9.5 nM 8.02
CHEMBL102527 IC50 = 9.8 nM 8.01
CHEMBL292748 IC50 = 11.0 nM 7.96
CHEMBL319463 IC50 = 23.0 nM 7.64
CHEMBL421021 IC50 = 24.0 nM 7.62
CHEMBL102815 IC50 = 27.0 nM 7.57
CHEMBL103327 IC50 = 30.0 nM 7.52
CHEMBL419170 IC50 = 39.0 nM 7.41
CHEMBL421586 IC50 = 41.0 nM 7.39
CHEMBL105054 IC50 = 43.0 nM 7.37
CHEMBL320400 IC50 = 49.0 nM 7.31
CHEMBL103378 IC50 = 55.0 nM 7.26
CHEMBL104617 IC50 = 56.0 nM 7.25
CHEMBL103966 IC50 = 64.0 nM 7.19
CHEMBL64081 IC50 = 77.0 nM 7.11
CHEMBL104814 IC50 = 77.0 nM 7.11
CHEMBL102795 IC50 = 82.0 nM 7.09
CHEMBL320471 IC50 = 98.0 nM 7.01
CHEMBL319708 IC50 = 120.0 nM 6.92
CHEMBL419725 IC50 = 130.0 nM 6.89
CHEMBL441817 IC50 = 700.0 nM 6.16