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Assay Detail

CHEMBL2185058

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

Binding
Inhibition of porcine kidney microsomal neutral aminopeptidase using Leu-pNA as substrate preincubated for 10 mins
13
Total Activities
13
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

Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors.
Deprez-Poulain R, Flipo M, Piveteau C, Leroux F, Dassonneville S, Florent I, Maes L, Cos P, Deprez B.
J Med Chem (2012) 55 : 10909 -10917
PubMed 23176597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.59 5.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180993 1 5.88
CHEMBL219777 1 5.86
CHEMBL2180998 1 5.70
CHEMBL2180992 1 5.65
CHEMBL2180991 1 5.63
CHEMBL2180995 1 5.62
CHEMBL219618 1 5.44
CHEMBL2180994 1 5.40
CHEMBL2180996 1 5.38
CHEMBL2180997 1 5.34
CHEMBL572368 1 -
CHEMBL113827 1 -
CHEMBL376895 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180993 IC50 = 1324.0 nM 5.88
CHEMBL219777 IC50 = 1372.0 nM 5.86
CHEMBL2180998 IC50 = 2000.0 nM 5.70
CHEMBL2180992 IC50 = 2223.0 nM 5.65
CHEMBL2180991 IC50 = 2333.0 nM 5.63
CHEMBL2180995 IC50 = 2400.0 nM 5.62
CHEMBL219618 IC50 = 3616.0 nM 5.44
CHEMBL2180994 IC50 = 3956.0 nM 5.40
CHEMBL2180996 IC50 = 4200.0 nM 5.38
CHEMBL2180997 IC50 = 4550.0 nM 5.34
CHEMBL572368 IC50 > 10000.0 nM -
CHEMBL113827 IC50 > 10000.0 nM -
CHEMBL376895 IC50 > 10000.0 nM -