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Compound Detail

CHEMBL2385287

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N#C[C@@H]1CCCN1C(=O)COc1cccc2ccccc12

Basic Information

ChEMBL ID CHEMBL2385287
Phase Preclinical
Structure Type MOL
InChI Key GXTNNLMFNYTVNV-AWEZNQCLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

280.3
MW (Da)
2.73
ALogP
3
HBA
0
HBD
53.3
PSA (Ų)
0.87
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H16N2O2
MW 280.33
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prolyl endopeptidase
CHEMBL3202
IC50 4.48 4.48 33000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prolyl endopeptidase IC50 = 33000.0 nM 4.48 Inhibition of human recombinant PREP expressed in Escherichia coli using Z-Gly-P... 24900696

Literature References

PubMed DOI Target Context # Activities
24900696 10.1021/ml300410d Prolyl endopeptidase 1
24900696 10.1021/ml300410d Dipeptidyl peptidase 2 1
24900696 10.1021/ml300410d Unchecked 1
24900696 10.1021/ml300410d Dipeptidyl peptidase 4 1
24900696 10.1021/ml300410d Prolyl endopeptidase FAP 1

Data from ChEMBL 36 via Core Engine