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Assay Detail

CHEMBL765788

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Binding
Inhibition of Prolyl endopeptidase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.
Vendeville S, Bourel L, Davioud-Charvet E, Grellier P, Deprez B, Sergheraert C.
Bioorg Med Chem Lett (1999) 9 : 437 -442
PubMed 10091698 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.68 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335796 1 8.15
CHEMBL139862 1 8.05
CHEMBL422281 1 7.85
CHEMBL289651 1 7.82
CHEMBL342718 1 7.77
CHEMBL342651 1 7.68
CHEMBL138674 1 7.68
CHEMBL139696 1 7.64
CHEMBL423002 1 7.60
CHEMBL136325 1 7.44
CHEMBL334569 1 7.27
CHEMBL341749 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335796 IC50 = 7.0 nM 8.15
CHEMBL139862 IC50 = 9.0 nM 8.05
CHEMBL422281 IC50 = 14.0 nM 7.85
CHEMBL289651 IC50 = 15.0 nM 7.82
CHEMBL342718 IC50 = 17.0 nM 7.77
CHEMBL342651 IC50 = 21.0 nM 7.68
CHEMBL138674 IC50 = 21.0 nM 7.68
CHEMBL139696 IC50 = 23.0 nM 7.64
CHEMBL423002 IC50 = 25.0 nM 7.60
CHEMBL136325 IC50 = 36.0 nM 7.44
CHEMBL334569 IC50 = 54.0 nM 7.27
CHEMBL341749 IC50 = 55.0 nM 7.26