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Assay Detail

CHEMBL765791

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

Binding
In vitro inhibitory activity against purified prolyl endopeptidase (PEP) from canine brain.
37
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prolyl endopeptidase (CHEMBL3202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues.
Tanaka Y, Niwa S, Nishioka H, Yamanaka T, Torizuka M, Yoshinaga K, Kobayashi N, Ikeda Y, Arai H.
J Med Chem (1994) 37 : 2071 -2078
PubMed 8027988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.61 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302654 1 9.38
CHEMBL65284 1 9.35
CHEMBL291393 1 9.34
CHEMBL63745 1 9.28
CHEMBL294367 1 9.26
CHEMBL65512 1 9.07
CHEMBL65338 1 9.00
CHEMBL79993 Z-PRO-PROLINAL 1 8.96
CHEMBL66088 1 8.96
CHEMBL62580 1 8.92
CHEMBL304644 1 8.64
CHEMBL65109 1 8.47
CHEMBL66257 1 8.40
CHEMBL63045 1 8.27
CHEMBL66258 1 8.19
CHEMBL64240 1 8.06
CHEMBL62960 1 8.00
CHEMBL262241 1 7.77
CHEMBL304020 1 7.75
CHEMBL63133 1 7.62
CHEMBL303066 1 7.44
CHEMBL63994 1 7.42
CHEMBL63537 1 7.40
CHEMBL292302 1 7.32
CHEMBL289651 1 7.31
CHEMBL416866 1 7.22
CHEMBL65373 1 7.16
CHEMBL23089 1 7.07
CHEMBL293168 1 6.89
CHEMBL413107 2 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302654 IC50 = 0.42 nM 9.38
CHEMBL65284 IC50 = 0.45 nM 9.35
CHEMBL291393 IC50 = 0.46 nM 9.34
CHEMBL63745 IC50 = 0.52 nM 9.28
CHEMBL294367 IC50 = 0.55 nM 9.26
CHEMBL65512 IC50 = 0.85 nM 9.07
CHEMBL65338 IC50 = 1.0 nM 9.00
CHEMBL79993 Z-PRO-PROLINAL IC50 = 1.1 nM 8.96
CHEMBL66088 IC50 = 1.1 nM 8.96
CHEMBL62580 IC50 = 1.2 nM 8.92
CHEMBL304644 IC50 = 2.3 nM 8.64
CHEMBL65109 IC50 = 3.4 nM 8.47
CHEMBL66257 IC50 = 4.0 nM 8.40
CHEMBL63045 IC50 = 5.4 nM 8.27
CHEMBL66258 IC50 = 6.5 nM 8.19
CHEMBL64240 IC50 = 8.7 nM 8.06
CHEMBL62960 IC50 = 10.0 nM 8.00
CHEMBL262241 IC50 = 17.0 nM 7.77
CHEMBL304020 IC50 = 18.0 nM 7.75
CHEMBL63133 IC50 = 24.0 nM 7.62
CHEMBL303066 IC50 = 36.0 nM 7.44
CHEMBL63994 IC50 = 38.0 nM 7.42
CHEMBL63537 IC50 = 40.0 nM 7.40
CHEMBL292302 IC50 = 48.0 nM 7.32
CHEMBL289651 IC50 = 49.0 nM 7.31
CHEMBL416866 IC50 = 60.0 nM 7.22
CHEMBL65373 IC50 = 69.0 nM 7.16
CHEMBL23089 IC50 = 86.0 nM 7.07
CHEMBL293168 IC50 = 130.0 nM 6.89
CHEMBL413107 IC50 = 150.0 nM 6.82
CHEMBL413107 IC50 = 250.0 nM 6.60
CHEMBL304892 IC50 = 510.0 nM 6.29
CHEMBL62629 IC50 = 520.0 nM 6.28
CHEMBL294803 IC50 = 3500.0 nM 5.46
CHEMBL65463 IC50 = 80000.0 nM 4.10
CHEMBL65561 IC50 = 91000.0 nM 4.04
CHEMBL302398 IC50 = 94000.0 nM 4.03