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Compound Detail

CHEMBL511659

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CC[C@@H](C)[C@H](N)C(=O)N1C[C@H](N=[N+]=[N-])C[C@H]1C#N

Basic Information

ChEMBL ID CHEMBL511659
Phase Preclinical
Structure Type MOL
InChI Key QZBJOAGVNBRVQF-IMSYWVGJSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

250.3
MW (Da)
1.16
ALogP
4
HBA
1
HBD
118.9
PSA (Ų)
0.46
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 C11H18N6O
MW 250.31
Aromatic Rings 0
Heavy Atoms 18
NP-Likeness 0.25

Activity Summary

IC50 4 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.04 5.04 9200.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.66 4.66 22000.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 4.28 4.28 52000.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.05 4.05 90000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 9 IC50 = 9200.0 nM 5.04 Inhibition of DPP9 18556199
Dipeptidyl peptidase 8 IC50 = 22000.0 nM 4.66 Inhibition of DPP8 18556199
Dipeptidyl peptidase 4 IC50 = 52000.0 nM 4.28 Inhibition of DPP4 18556199
Dipeptidyl peptidase 2 IC50 = 90000.0 nM 4.05 Inhibition of DPP2 18556199

Literature References

PubMed DOI Target Context # Activities
28826083 10.1016/j.ejmech.2017.08.024 Dipeptidyl peptidase IV 3
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