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Assay Detail

CHEMBL2160636

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

Binding
Inhibition of POP in intact human LN229 cells using Cbz-Gly-Pro-AMC substrate incubated for 30 mins by fluorimetric assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LN229
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Virtual screening and computational optimization for the discovery of covalent prolyl oligopeptidase inhibitors with activity in human cells.
De Cesco S, Deslandes S, Therrien E, Levan D, Cueto M, Schmidt R, Cantin LD, Mittermaier A, Juillerat-Jeanneret L, Moitessier N.
J Med Chem (2012) 55 : 6306 -6315
PubMed 22765237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.29 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159748 1 6.35
CHEMBL2159745 1 6.30
CHEMBL2159749 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159748 IC50 = 450.0 nM 6.35
CHEMBL2159745 IC50 = 500.0 nM 6.30
CHEMBL2159749 IC50 = 610.0 nM 6.21