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Assay Detail

CHEMBL998642

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

Binding
Inhibition of POP in Sprague-Dawley rat brain homogenates
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase (CHEMBL4035)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Prolyl oligopeptidase inhibition by N-acyl-pro-pyrrolidine-type molecules.
Kánai K, Arányi P, Böcskei Z, Ferenczy G, Harmat V, Simon K, Bátori S, Náray-Szabo G, Hermecz I.
J Med Chem (2008) 51 : 7514 -7522
PubMed 19006380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.94 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458975 1 9.09
CHEMBL459149 1 9.06
CHEMBL515056 1 8.52
CHEMBL45594 1 7.96
CHEMBL289651 1 7.52
CHEMBL458976 1 7.40
CHEMBL516159 1 7.39
CHEMBL298028 1 7.32
CHEMBL457904 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458975 IC50 = 0.81 nM 9.09
CHEMBL459149 IC50 = 0.88 nM 9.06
CHEMBL515056 IC50 = 3.0 nM 8.52
CHEMBL45594 IC50 = 11.0 nM 7.96
CHEMBL289651 IC50 = 30.0 nM 7.52
CHEMBL458976 IC50 = 40.0 nM 7.40
CHEMBL516159 IC50 = 41.0 nM 7.39
CHEMBL298028 IC50 = 48.0 nM 7.32
CHEMBL457904 IC50 = 59.0 nM 7.23