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Assay Detail

CHEMBL646206

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Binding
Inhibition of aminopeptidase A (APA)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamyl aminopeptidase (CHEMBL3439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors.
Chauvel EN, Coric P, Llorens-Cortès C, Wilk S, Roques BP, Fournié-Zaluski MC.
J Med Chem (1994) 37 : 1339 -1346
PubMed 7909847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.78 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28124 1 6.85
CHEMBL283227 1 6.08
CHEMBL27824 1 6.06
CHEMBL26376 1 5.72
CHEMBL26032 1 5.70
CHEMBL282364 1 5.66
CHEMBL27656 1 5.64
CHEMBL281321 1 5.62
CHEMBL25915 1 5.57
CHEMBL27040 1 5.55
CHEMBL28650 AMASTATIN 1 5.10
CHEMBL27519 1 -
CHEMBL26382 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28124 Ki = 140.0 nM 6.85
CHEMBL283227 Ki = 840.0 nM 6.08
CHEMBL27824 Ki = 870.0 nM 6.06
CHEMBL26376 Ki = 1900.0 nM 5.72
CHEMBL26032 Ki = 2000.0 nM 5.70
CHEMBL282364 Ki = 2200.0 nM 5.66
CHEMBL27656 Ki = 2300.0 nM 5.64
CHEMBL281321 Ki = 2400.0 nM 5.62
CHEMBL25915 Ki = 2700.0 nM 5.57
CHEMBL27040 Ki = 2800.0 nM 5.55
CHEMBL28650 AMASTATIN Ki = 8000.0 nM 5.10
CHEMBL27519 Ki > 3000.0 nM -
CHEMBL26382 Ki > 3000.0 nM -