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Assay Detail

CHEMBL1045249

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

Binding
Inhibition of human somatic ECE1
17
Total Activities
17
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

Endothelin-converting enzyme 1 (CHEMBL4791)
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 7.33 8.92
IC50 3 6.89 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571153 1 8.92
CHEMBL567628 1 8.11
CHEMBL577754 1 8.10
CHEMBL570953 1 7.85
CHEMBL570843 1 7.85
CHEMBL146936 1 7.66
CHEMBL577753 1 7.58
CHEMBL43370 1 7.10
CHEMBL570718 1 6.62
CHEMBL570732 1 6.56
CHEMBL570842 1 6.04
CHEMBL479579 PHOSPHORAMIDON 1 5.92
CHEMBL570811 1 5.68
CHEMBL570722 1 -
CHEMBL570740 1 -
CHEMBL570704 1 -
CHEMBL571716 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571153 Ki = 1.2 nM 8.92
CHEMBL567628 Ki = 7.7 nM 8.11
CHEMBL577754 Ki = 8.0 nM 8.10
CHEMBL570953 Ki = 14.0 nM 7.85
CHEMBL570843 Ki = 14.0 nM 7.85
CHEMBL146936 IC50 = 22.0 nM 7.66
CHEMBL577753 Ki = 26.0 nM 7.58
CHEMBL43370 IC50 = 80.0 nM 7.10
CHEMBL570718 Ki = 240.0 nM 6.62
CHEMBL570732 Ki = 275.0 nM 6.56
CHEMBL570842 Ki = 910.0 nM 6.04
CHEMBL479579 PHOSPHORAMIDON IC50 = 1200.0 nM 5.92
CHEMBL570811 Ki = 2100.0 nM 5.68
CHEMBL570722 Ki > 10000.0 nM -
CHEMBL570740 Ki > 10000.0 nM -
CHEMBL570704 Ki > 5000.0 nM -
CHEMBL571716 Ki > 50000.0 nM -