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Assay Detail

CHEMBL874110

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

Binding
Compound was evaluated for the inhibition of Aminopeptidase M (AP-M) and the inhibition constant was determined after preincubating the enzyme and inhibitor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aminopeptidase N (CHEMBL2590)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
Rich DH, Moon BJ, Harbeson S.
J Med Chem (1984) 27 : 417 -423
PubMed 6142952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.77 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28650 AMASTATIN 1 7.70
CHEMBL3143143 1 6.75
CHEMBL134414 1 6.03
CHEMBL1689155 1 4.93
CHEMBL2370765 1 4.60
CHEMBL2370764 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28650 AMASTATIN Ki = 20.0 nM 7.70
CHEMBL3143143 Ki = 180.0 nM 6.75
CHEMBL134414 Ki = 940.0 nM 6.03
CHEMBL1689155 Ki = 11760.0 nM 4.93
CHEMBL2370765 Ki = 25000.0 nM 4.60
CHEMBL2370764 Ki = 26000.0 nM 4.58