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Assay Detail

CHEMBL878424

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

Binding
Inhibitory activity against rat brain Prolyl endopeptidase (PEP)
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prolyl endopeptidase (CHEMBL4035)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Prolyl endopeptidase inhibitors1: N-acyl derivatives of L-thioproline-pyrrolidine
Karoly K, Sandor E, Edit S, Miklos F, Judit S, Benjamin P, Andrea S, Istvan H
Bioorg Med Chem Lett (1997) 7 : 1701 -1704
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.17 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45594 1 7.96
CHEMBL44744 1 7.77
CHEMBL298028 1 7.70
CHEMBL289651 1 7.52
CHEMBL417354 1 7.47
CHEMBL47990 1 7.43
CHEMBL44745 1 7.43
CHEMBL296645 1 7.42
CHEMBL47565 1 7.42
CHEMBL48005 1 7.38
CHEMBL47927 1 7.34
CHEMBL297237 1 7.14
CHEMBL47926 1 7.10
CHEMBL45684 1 6.98
CHEMBL47932 1 6.78
CHEMBL45668 1 6.68
CHEMBL50765 1 6.67
CHEMBL50764 1 6.04
CHEMBL47936 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45594 IC50 = 11.0 nM 7.96
CHEMBL44744 IC50 = 17.0 nM 7.77
CHEMBL298028 IC50 = 20.0 nM 7.70
CHEMBL289651 IC50 = 30.0 nM 7.52
CHEMBL417354 IC50 = 34.0 nM 7.47
CHEMBL47990 IC50 = 37.0 nM 7.43
CHEMBL44745 IC50 = 37.0 nM 7.43
CHEMBL296645 IC50 = 38.0 nM 7.42
CHEMBL47565 IC50 = 38.0 nM 7.42
CHEMBL48005 IC50 = 42.0 nM 7.38
CHEMBL47927 IC50 = 46.0 nM 7.34
CHEMBL297237 IC50 = 73.0 nM 7.14
CHEMBL47926 IC50 = 80.0 nM 7.10
CHEMBL45684 IC50 = 104.0 nM 6.98
CHEMBL47932 IC50 = 167.0 nM 6.78
CHEMBL45668 IC50 = 207.0 nM 6.68
CHEMBL50765 IC50 = 216.0 nM 6.67
CHEMBL50764 IC50 = 904.0 nM 6.04
CHEMBL47936 IC50 = 1157.0 nM 5.94