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Compound Detail

CHEMBL200347

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N#C[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(-c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL200347
Phase Preclinical
Structure Type MOL
InChI Key JFHXVIXBGWKRGK-OALUTQOASA-N
5
Targets
6
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
2.74
ALogP
3
HBA
1
HBD
70.1
PSA (Ų)
0.94
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21N3O
MW 319.41
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.30

Activity Summary

IC50 5 meas. best 6.84
Ki 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
Ki 7.89 7.89 13.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.84 6.84 145.0 1
Prolyl endopeptidase FAP
CHEMBL4683
IC50 5.85 5.85 1410.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.46 5.46 3440.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.38 5.38 4130.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.03 5.03 9420.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24153396 10.1016/j.bmc.2013.09.048 Unchecked 3
16236500 10.1016/j.bmcl.2005.09.037 Caco-2 2
16236500 10.1016/j.bmcl.2005.09.037 Dipeptidyl peptidase 4 1
16236500 10.1016/j.bmcl.2005.09.037 Liver microsomes 1
24153396 10.1016/j.bmc.2013.09.048 Prolyl endopeptidase FAP 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 9 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 8 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 2 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine