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Compound Detail

CHEMBL482262

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N#C[C@@H]1C[C@H](F)CN1C(=O)CN[C@H]1[C@@H]2CN(c3nccc(C(F)(F)F)n3)C[C@@H]21

Basic Information

ChEMBL ID CHEMBL482262
Phase Preclinical
Structure Type MOL
InChI Key CCAHGNFSCCVYCY-QHUBEEEXSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

398.4
MW (Da)
0.98
ALogP
6
HBA
1
HBD
85.2
PSA (Ų)
0.76
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 C17H18F4N6O
MW 398.36
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.98

Activity Summary

IC50 4 meas. best 6.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.74 6.74 181.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.66 5.66 2200.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.27 5.27 5420.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.96 4.96 11100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 181.0 nM 6.74 Inhibition of human plasma DPP4 18602260
Dipeptidyl peptidase 2 IC50 = 2200.0 nM 5.66 Inhibition of DPP2 18602260
Dipeptidyl peptidase 9 IC50 = 5420.0 nM 5.27 Inhibition of DPP9 18602260
Dipeptidyl peptidase 8 IC50 = 11100.0 nM 4.96 Inhibition of DPP8 18602260

Literature References

PubMed DOI Target Context # Activities
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

Data from ChEMBL 36 via Core Engine