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Assay Detail

CHEMBL675441

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

Binding
In vitro inhibition of human Endothelin converting Enzyme-1 activity
16
Total Activities
16
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

Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1.
Fink CA, Moskal M, Firooznia F, Hoyer D, Symonsbergen D, Wei D, Qiao Y, Savage P, Beil ME, Trapani AJ, Jeng AY.
Bioorg Med Chem Lett (2000) 10 : 2037 -2039
PubMed 10987444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.01 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293024 1 7.96
CHEMBL292748 1 7.96
CHEMBL61269 1 7.72
CHEMBL61410 1 7.40
CHEMBL292733 1 7.27
CHEMBL64081 1 7.11
CHEMBL2115491 1 7.01
CHEMBL3351079 1 6.92
CHEMBL63132 1 6.85
CHEMBL304408 1 6.77
CHEMBL292044 1 6.70
CHEMBL303775 1 6.68
CHEMBL303570 1 6.62
CHEMBL59775 1 6.55
CHEMBL2114468 1 6.39
CHEMBL60679 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293024 IC50 = 11.0 nM 7.96
CHEMBL292748 IC50 = 11.0 nM 7.96
CHEMBL61269 IC50 = 19.0 nM 7.72
CHEMBL61410 IC50 = 40.0 nM 7.40
CHEMBL292733 IC50 = 54.0 nM 7.27
CHEMBL64081 IC50 = 77.0 nM 7.11
CHEMBL2115491 IC50 = 97.0 nM 7.01
CHEMBL3351079 IC50 = 120.0 nM 6.92
CHEMBL63132 IC50 = 140.0 nM 6.85
CHEMBL304408 IC50 = 170.0 nM 6.77
CHEMBL292044 IC50 = 200.0 nM 6.70
CHEMBL303775 IC50 = 210.0 nM 6.68
CHEMBL303570 IC50 = 240.0 nM 6.62
CHEMBL59775 IC50 = 280.0 nM 6.55
CHEMBL2114468 IC50 = 410.0 nM 6.39
CHEMBL60679 IC50 = 510.0 nM 6.29