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Assay Detail

CHEMBL675453

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

Binding
Inhibition of Endothelin-converting enzyme (ECE) from microsomal fractions of bovine cultured endothelial cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Cell Type Endothelial cell
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin-converting enzyme 1 (CHEMBL2340)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon
Fukami T, Hayama T, Amano Y, Nakamura Y, Arai Y, Matsuyama K, Yano M, Ishikawa K
Bioorg Med Chem Lett (1994) 4 : 1257 -1262
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.60 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25269 1 6.58
CHEMBL281562 1 6.02
CHEMBL277199 1 5.96
CHEMBL22509 1 5.82
CHEMBL283758 1 5.72
CHEMBL281785 1 5.55
CHEMBL282663 1 5.52
CHEMBL479579 PHOSPHORAMIDON 1 5.51
CHEMBL281333 1 5.47
CHEMBL277195 1 5.15
CHEMBL280917 1 5.13
CHEMBL279255 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25269 IC50 = 260.0 nM 6.58
CHEMBL281562 IC50 = 960.0 nM 6.02
CHEMBL277199 IC50 = 1100.0 nM 5.96
CHEMBL22509 IC50 = 1500.0 nM 5.82
CHEMBL283758 IC50 = 1900.0 nM 5.72
CHEMBL281785 IC50 = 2800.0 nM 5.55
CHEMBL282663 IC50 = 3000.0 nM 5.52
CHEMBL479579 PHOSPHORAMIDON IC50 = 3100.0 nM 5.51
CHEMBL281333 IC50 = 3400.0 nM 5.47
CHEMBL277195 IC50 = 7100.0 nM 5.15
CHEMBL280917 IC50 = 7400.0 nM 5.13
CHEMBL279255 IC50 = 15000.0 nM 4.82