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Assay Detail

CHEMBL675914

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

Binding
Inhibition of Endothelin-converting enzyme of guinea pig lung membrane
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Lung
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Highly potent and selective inhibitors of endothelin converting enzyme
Chackalamannil S, Chung S, Stamford AW, McKittrick BA, Wang Y, Tsai H, Cleven R, Fawzi A, Czarniecki M
Bioorg Med Chem Lett (1996) 6 : 1257 -1260
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.47 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22957 1 7.60
CHEMBL282660 1 7.40
CHEMBL280152 1 7.19
CHEMBL479579 PHOSPHORAMIDON 1 7.00
CHEMBL278076 1 6.80
CHEMBL427799 1 6.60
CHEMBL25221 1 6.41
CHEMBL23598 1 6.30
CHEMBL280907 1 6.30
CHEMBL435561 1 6.10
CHEMBL262783 2 5.89
CHEMBL18461 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22957 IC50 = 25.0 nM 7.60
CHEMBL282660 IC50 = 40.0 nM 7.40
CHEMBL280152 IC50 = 65.0 nM 7.19
CHEMBL479579 PHOSPHORAMIDON IC50 = 100.0 nM 7.00
CHEMBL278076 IC50 = 160.0 nM 6.80
CHEMBL427799 IC50 = 250.0 nM 6.60
CHEMBL25221 IC50 = 390.0 nM 6.41
CHEMBL23598 IC50 = 500.0 nM 6.30
CHEMBL280907 IC50 = 500.0 nM 6.30
CHEMBL435561 IC50 = 800.0 nM 6.10
CHEMBL262783 IC50 = 1300.0 nM 5.89
CHEMBL18461 IC50 = 5000.0 nM 5.30
CHEMBL262783 IC50 = 6000.0 nM 5.22