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Compound Detail

CHEMBL2425069

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N[C@H]1C[C@@H](N2Cc3nc(C(F)(F)F)[nH]c3C2)CO[C@@H]1c1cc(F)ccc1F

Basic Information

ChEMBL ID CHEMBL2425069
Phase Preclinical
Structure Type MOL
InChI Key NRTUDFQDPVFTRM-MURWCNHISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

388.3
MW (Da)
2.88
ALogP
4
HBA
2
HBD
67.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17F5N4O
MW 388.34
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.66

Activity Summary

IC50 2 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.8 8.8 1.6 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.66 6.66 220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 1.6 nM 8.8 Inhibition of human DPP4 23972441
Dipeptidyl peptidase 8 IC50 = 220.0 nM 6.66 Inhibition of human DPP8 23972441

Literature References

PubMed DOI Target Context # Activities
23972441 10.1016/j.bmcl.2013.07.061 Prolyl endopeptidase FAP 1
23972441 10.1016/j.bmcl.2013.07.061 Dipeptidyl peptidase 2 1
23972441 10.1016/j.bmcl.2013.07.061 Dipeptidyl peptidase 8 1
23972441 10.1016/j.bmcl.2013.07.061 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine