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Assay Detail

CHEMBL1045247

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

Binding
Inhibition of human somatic ACE C-terminal domain
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Angiotensin-converting enzyme (CHEMBL1808)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
Jullien N, Makritis A, Georgiadis D, Beau F, Yiotakis A, Dive V.
J Med Chem (2010) 53 : 208 -220
PubMed 19899765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.40 9.40
IC50 1 8.60 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570718 1 9.40
CHEMBL570732 1 9.39
CHEMBL570953 1 9.19
CHEMBL577753 1 8.85
CHEMBL43370 1 8.60
CHEMBL571716 1 8.52
CHEMBL577754 1 8.44
CHEMBL567628 1 8.42
CHEMBL570811 1 8.30
CHEMBL289556 OMAPATRILAT 2.0 1 8.22
CHEMBL570740 1 7.92
CHEMBL570842 1 7.89
CHEMBL570843 1 7.80
CHEMBL570704 1 7.70
CHEMBL570722 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570718 Ki = 0.4 nM 9.40
CHEMBL570732 Ki = 0.41 nM 9.39
CHEMBL570953 Ki = 0.65 nM 9.19
CHEMBL577753 Ki = 1.4 nM 8.85
CHEMBL43370 IC50 = 2.5 nM 8.60
CHEMBL571716 Ki = 3.0 nM 8.52
CHEMBL577754 Ki = 3.6 nM 8.44
CHEMBL567628 Ki = 3.8 nM 8.42
CHEMBL570811 Ki = 5.0 nM 8.30
CHEMBL289556 OMAPATRILAT Ki = 6.0 nM 8.22
CHEMBL570740 Ki = 12.0 nM 7.92
CHEMBL570842 Ki = 13.0 nM 7.89
CHEMBL570843 Ki = 16.0 nM 7.80
CHEMBL570704 Ki = 20.0 nM 7.70
CHEMBL570722 Ki = 25.0 nM 7.60