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Assay Detail

CHEMBL644740

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

Binding
In vitro inhibition of ACE (Angiotensin I converting enzyme) isolated from rabbit lung extract
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Angiotensin-converting enzyme (CHEMBL4074)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics as inhibitors of angiotensin-converting enzyme and neutral endopeptidase.
Robl JA, Sun CQ, Stevenson J, Ryono DE, Simpkins LM, Cimarusti MP, Dejneka T, Slusarchyk WA, Chao S, Stratton L, Misra RN, Bednarz MS, Asaad MM, Cheung HS, Abboa-Offei BE, Smith PL, Mathers PD, Fox M, Schaeffer TR, Seymour AA, Trippodo NC.
J Med Chem (1997) 40 : 1570 -1577
PubMed 9171867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.13 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41753 1 8.40
CHEMBL39774 1 8.30
CHEMBL289556 OMAPATRILAT 2.0 1 8.30
CHEMBL41201 1 8.30
CHEMBL289534 1 8.15
CHEMBL290754 1 8.10
CHEMBL39775 1 7.96
CHEMBL287896 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41753 IC50 = 4.0 nM 8.40
CHEMBL39774 IC50 = 5.0 nM 8.30
CHEMBL289556 OMAPATRILAT IC50 = 5.0 nM 8.30
CHEMBL41201 IC50 = 5.0 nM 8.30
CHEMBL289534 IC50 = 7.0 nM 8.15
CHEMBL290754 IC50 = 8.0 nM 8.10
CHEMBL39775 IC50 = 11.0 nM 7.96
CHEMBL287896 IC50 = 30.0 nM 7.52