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Assay Detail

CHEMBL679847

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

Binding
Inhibitory activity was assessed on CHO cells expressing recombinant human Endothelin-converting enzyme 1 (ECE-1).
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
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, selective inhibitors of endothelin-converting enzyme.
Wallace EM, Moliterni JA, Moskal MA, Neubert AD, Marcopulos N, Stamford LB, Trapani AJ, Savage P, Chou M, Jeng AY.
J Med Chem (1998) 41 : 1513 -1523
PubMed 9554884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.97 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147847 1 8.10
CHEMBL37052 1 7.89
CHEMBL39828 1 7.85
CHEMBL285619 1 7.77
CHEMBL39887 1 7.60
CHEMBL40168 1 7.55
CHEMBL39777 1 7.55
CHEMBL39714 1 7.48
CHEMBL290868 1 7.47
CHEMBL416234 1 7.37
CHEMBL289150 1 7.29
CHEMBL37078 1 7.28
CHEMBL37542 1 7.25
CHEMBL290304 1 7.12
CHEMBL446393 1 7.09
CHEMBL289638 1 6.96
CHEMBL36382 1 6.96
CHEMBL417507 1 6.96
CHEMBL35995 1 6.96
CHEMBL290256 1 6.92
CHEMBL36809 1 6.89
CHEMBL287971 1 6.85
CHEMBL290332 1 6.82
CHEMBL40028 1 6.82
CHEMBL290287 1 6.80
CHEMBL39812 1 6.77
CHEMBL36753 1 6.64
CHEMBL39997 1 6.64
CHEMBL448098 1 6.62
CHEMBL37861 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147847 IC50 = 8.0 nM 8.10
CHEMBL37052 IC50 = 13.0 nM 7.89
CHEMBL39828 IC50 = 14.0 nM 7.85
CHEMBL285619 IC50 = 17.0 nM 7.77
CHEMBL39887 IC50 = 25.0 nM 7.60
CHEMBL40168 IC50 = 28.0 nM 7.55
CHEMBL39777 IC50 = 28.0 nM 7.55
CHEMBL39714 IC50 = 33.0 nM 7.48
CHEMBL290868 IC50 = 34.0 nM 7.47
CHEMBL416234 IC50 = 43.0 nM 7.37
CHEMBL289150 IC50 = 51.0 nM 7.29
CHEMBL37078 IC50 = 53.0 nM 7.28
CHEMBL37542 IC50 = 56.0 nM 7.25
CHEMBL290304 IC50 = 76.0 nM 7.12
CHEMBL446393 IC50 = 82.0 nM 7.09
CHEMBL36382 IC50 = 110.0 nM 6.96
CHEMBL417507 IC50 = 110.0 nM 6.96
CHEMBL289638 IC50 = 110.0 nM 6.96
CHEMBL35995 IC50 = 111.0 nM 6.96
CHEMBL290256 IC50 = 120.0 nM 6.92
CHEMBL36809 IC50 = 130.0 nM 6.89
CHEMBL287971 IC50 = 140.0 nM 6.85
CHEMBL290332 IC50 = 150.0 nM 6.82
CHEMBL40028 IC50 = 150.0 nM 6.82
CHEMBL290287 IC50 = 160.0 nM 6.80
CHEMBL39812 IC50 = 170.0 nM 6.77
CHEMBL39997 IC50 = 230.0 nM 6.64
CHEMBL36753 IC50 = 230.0 nM 6.64
CHEMBL448098 IC50 = 240.0 nM 6.62
CHEMBL37861 IC50 = 250.0 nM 6.60
CHEMBL37456 IC50 = 310.0 nM 6.51
CHEMBL434208 IC50 = 400.0 nM 6.40
CHEMBL290698 IC50 = 410.0 nM 6.39
CHEMBL288837 IC50 = 510.0 nM 6.29
CHEMBL39384 IC50 = 590.0 nM 6.23
CHEMBL479579 PHOSPHORAMIDON IC50 = 1200.0 nM 5.92
CHEMBL40161 IC50 = 4300.0 nM 5.37