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Assay Detail

CHEMBL673751

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Binding
In vitro inhibitory activity was tested against Endothelin converting enzyme 1
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

Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors.
Firooznia F, Gude C, Chan K, Fink CA, Qiao Y, Satoh Y, Marcopoulos N, Savage P, Beil ME, Bruseo CW, Trapani AJ, Jeng AY.
Bioorg Med Chem Lett (2001) 11 : 375 -378
PubMed 11212114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.56 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292748 1 7.96
CHEMBL319708 1 6.92
CHEMBL330896 1 6.89
CHEMBL124766 1 6.82
CHEMBL121821 1 6.75
CHEMBL420915 1 6.66
CHEMBL125234 1 6.52
CHEMBL125593 1 6.50
CHEMBL331080 1 6.46
CHEMBL121856 1 6.43
CHEMBL125655 1 6.31
CHEMBL331531 1 6.25
CHEMBL125987 1 6.19
CHEMBL126045 1 6.19
CHEMBL125174 1 6.09
CHEMBL124132 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292748 IC50 = 11.0 nM 7.96
CHEMBL319708 IC50 = 120.0 nM 6.92
CHEMBL330896 IC50 = 130.0 nM 6.89
CHEMBL124766 IC50 = 150.0 nM 6.82
CHEMBL121821 IC50 = 180.0 nM 6.75
CHEMBL420915 IC50 = 220.0 nM 6.66
CHEMBL125234 IC50 = 300.0 nM 6.52
CHEMBL125593 IC50 = 320.0 nM 6.50
CHEMBL331080 IC50 = 350.0 nM 6.46
CHEMBL121856 IC50 = 370.0 nM 6.43
CHEMBL125655 IC50 = 490.0 nM 6.31
CHEMBL331531 IC50 = 560.0 nM 6.25
CHEMBL125987 IC50 = 650.0 nM 6.19
CHEMBL126045 IC50 = 650.0 nM 6.19
CHEMBL125174 IC50 = 810.0 nM 6.09
CHEMBL124132 IC50 = 990.0 nM 6.00