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Assay Detail

CHEMBL4194819

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

Binding
Inhibition of hog kidney APN using [3H]Tyr1-Leu5-enkephalin as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by liquid scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aminopeptidase N (CHEMBL2590)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Design of Aminopeptidase N Inhibitors as Anti-cancer Agents.
Amin SA, Adhikari N, Jha T.
J Med Chem (2018) 61 : 6468 -6490
PubMed 29630364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.32 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101771 1 7.50
CHEMBL27040 1 7.46
CHEMBL317189 1 7.43
CHEMBL28124 1 6.92
CHEMBL101147 1 6.48
CHEMBL282364 1 5.57
CHEMBL102006 1 4.81
CHEMBL4203901 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101771 Ki = 32.0 nM 7.50
CHEMBL27040 Ki = 35.0 nM 7.46
CHEMBL317189 Ki = 37.0 nM 7.43
CHEMBL28124 Ki = 120.0 nM 6.92
CHEMBL101147 Ki = 330.0 nM 6.48
CHEMBL282364 Ki = 2700.0 nM 5.57
CHEMBL102006 Ki = 15500.0 nM 4.81
CHEMBL4203901 Ki = 45000.0 nM 4.35