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Assay Detail

CHEMBL648453

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Binding
Inhibition of Angiotensin I converting enzyme
12
Total Activities
11
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

N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.
Robl JA, Simpkins LM, Asaad MM.
Bioorg Med Chem Lett (2000) 10 : 257 -260
PubMed 10698448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.87 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177551 1 8.47
CHEMBL90388 1 8.28
CHEMBL89533 1 8.27
CHEMBL289556 OMAPATRILAT 2.0 1 8.22
CHEMBL42583 SAMPATRILAT 2.0 1 8.15
CHEMBL89563 1 7.60
CHEMBL89760 2 7.03
CHEMBL314626 1 6.97
CHEMBL2370089 1 -
CHEMBL315395 1 -
CHEMBL88228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177551 IC50 = 3.4 nM 8.47
CHEMBL90388 IC50 = 5.3 nM 8.28
CHEMBL89533 IC50 = 5.4 nM 8.27
CHEMBL289556 OMAPATRILAT IC50 = 6.0 nM 8.22
CHEMBL42583 SAMPATRILAT IC50 = 7.0 nM 8.15
CHEMBL89563 IC50 = 25.0 nM 7.60
CHEMBL89760 IC50 = 93.0 nM 7.03
CHEMBL314626 IC50 = 106.0 nM 6.97
CHEMBL2370089 IC50 = 228000.0 nM -
CHEMBL315395 IC50 = 529000.0 nM -
CHEMBL88228 IC50 = 461000.0 nM -
CHEMBL89760 IC50 = 210000.0 nM -