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Assay Detail

CHEMBL4336751

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

Binding
Inhibition of recombinant human POP pre-incubated for 30 mins before addition of ZGP-pNA substrate by absorbance assay
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.
Plescia J, De Cesco S, Patrascu MB, Kurian J, Di Trani J, Dufresne C, Wahba AS, Janmamode N, Mittermaier AK, Moitessier N.
J Med Chem (2019) 62 : 7874 -7884
PubMed 31393718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.08 9.00
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL79993 Z-PRO-PROLINAL 1 9.00
CHEMBL4451993 1 8.40
CHEMBL2159748 1 7.60
CHEMBL4558566 1 6.96
CHEMBL2159749 1 6.80
CHEMBL4462021 1 6.77
CHEMBL4437462 1 6.54
CHEMBL4584206 1 6.21
CHEMBL4474579 1 5.48
CHEMBL4303429 1 -
CHEMBL4453293 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL79993 Z-PRO-PROLINAL Ki = 1.0 nM 9.00
CHEMBL4451993 Ki = 4.0 nM 8.40
CHEMBL2159748 Ki = 25.0 nM 7.60
CHEMBL4558566 Ki = 110.0 nM 6.96
CHEMBL2159749 Ki = 160.0 nM 6.80
CHEMBL4462021 Ki = 170.0 nM 6.77
CHEMBL4437462 Ki = 290.0 nM 6.54
CHEMBL4584206 Ki = 620.0 nM 6.21
CHEMBL4474579 Ki = 3300.0 nM 5.48
CHEMBL4303429 Inhibition - % -
CHEMBL4453293 Ki > 100000.0 nM -