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Assay Detail

CHEMBL1060018

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Binding
Inhibition of human recombinant ACE by fluorimetry
9
Total Activities
9
Compounds Tested
1
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

Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
Olimpieri F, Tambaro S, Fustero S, Lazzari P, Sanchez-Roselló M, Pani L, Volonterio A, Zanda M.
Bioorg Med Chem Lett (2009) 19 : 4715 -4719
PubMed 19596577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.73 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1560 CAPTOPRIL 4.0 1 9.92
CHEMBL540674 1 6.80
CHEMBL560409 1 6.55
CHEMBL551145 1 6.52
CHEMBL551622 1 6.40
CHEMBL560685 1 6.08
CHEMBL558146 1 6.00
CHEMBL367174 1 5.55
CHEMBL173287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1560 CAPTOPRIL IC50 = 0.12 nM 9.92
CHEMBL540674 IC50 = 160.0 nM 6.80
CHEMBL560409 IC50 = 280.0 nM 6.55
CHEMBL551145 IC50 = 300.0 nM 6.52
CHEMBL551622 IC50 = 400.0 nM 6.40
CHEMBL560685 IC50 = 830.0 nM 6.08
CHEMBL558146 IC50 = 1010.0 nM 6.00
CHEMBL367174 IC50 = 2800.0 nM 5.55
CHEMBL173287 IC50 > 10000.0 nM -