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Compound Detail

CHEMBL456298

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[N-]=[N+]=NC1CCN(C(=O)[C@@H](N)CCCCN)C1

Basic Information

ChEMBL ID CHEMBL456298
Phase Preclinical
Structure Type MOL
InChI Key SSCKJTXGMUKYBW-GKAPJAKFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

240.3
MW (Da)
0.35
ALogP
4
HBA
2
HBD
121.1
PSA (Ų)
0.30
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H20N6O
MW 240.31
Aromatic Rings 0
Heavy Atoms 17
NP-Likeness 0.23

Activity Summary

IC50 3 meas. best 5.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.31 5.31 4900.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.9 4.9 12500.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.58 4.58 26400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 2 IC50 = 4900.0 nM 5.31 Inhibition of DPP2 18556199
Dipeptidyl peptidase 8 IC50 = 12500.0 nM 4.9 Inhibition of DPP8 18556199
Dipeptidyl peptidase 9 IC50 = 26400.0 nM 4.58 Inhibition of DPP9 18556199

Literature References

PubMed DOI Target Context # Activities
18556199 10.1016/j.bmcl.2008.05.080 Dipeptidyl peptidase 8 1
18556199 10.1016/j.bmcl.2008.05.080 Dipeptidyl peptidase 9 1
18556199 10.1016/j.bmcl.2008.05.080 Dipeptidyl peptidase 4 1
18556199 10.1016/j.bmcl.2008.05.080 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine