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Compound Detail

CHEMBL511125

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N#C[C@@H]1C[C@H](F)CN1C(=O)CN[C@H]1[C@@H]2CN(c3ccccn3)C[C@@H]21

Basic Information

ChEMBL ID CHEMBL511125
Phase Preclinical
Structure Type MOL
InChI Key SGZSKDAIMPUTKY-CKENWRIRSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

329.4
MW (Da)
0.57
ALogP
5
HBA
1
HBD
72.3
PSA (Ų)
0.87
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 C17H20FN5O
MW 329.38
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -1.06

Activity Summary

IC50 4 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.57 7.57 27.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.08 6.08 837.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 5.85 5.85 1420.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.97 4.97 10800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 27.0 nM 7.57 Inhibition of human plasma DPP4 18602260
Dipeptidyl peptidase 8 IC50 = 837.0 nM 6.08 Inhibition of DPP8 18602260
Prolyl endopeptidase IC50 = 1420.0 nM 5.85 Inhibition of PPCE 18602260
Dipeptidyl peptidase 2 IC50 = 10800.0 nM 4.97 Inhibition of DPP2 18602260

Literature References

PubMed DOI Target Context # Activities
18602260 10.1016/j.bmcl.2008.05.101 Unchecked 3
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 4 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 2 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 8 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 9 1
18602260 10.1016/j.bmcl.2008.05.101 Prolyl endopeptidase 1
18602260 10.1016/j.bmcl.2008.05.101 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine