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Assay Detail

CHEMBL5042029

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

Binding
Inhibition of recombinant human ACE C-domain expressed in CHO cells using Cbz-Phe-His-Leu as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by fluorescence spectrophotometric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition.
Arendse LB, Cozier GE, Eyermann CJ, Basarab GS, Schwager SL, Chibale K, Acharya KR, Sturrock ED.
J Med Chem (2022) 65 : 3371 -3387
PubMed 35113565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.56 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1237 LISINOPRIL ANHYDROUS 4.0 1 8.92
CHEMBL212710 1 8.05
CHEMBL5077796 1 7.46
CHEMBL5075705 1 7.00
CHEMBL5075686 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1237 LISINOPRIL ANHYDROUS Ki = 1.2 nM 8.92
CHEMBL212710 Ki = 9.0 nM 8.05
CHEMBL5077796 Ki = 35.0 nM 7.46
CHEMBL5075705 Ki = 100.0 nM 7.00
CHEMBL5075686 Ki = 440.0 nM 6.36