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Compound Detail

CHEMBL2425081

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N[C@@H]1C[C@H](N2Cc3cn[nH]c3C2)CO[C@@H]1c1cc(F)ccc1F

Basic Information

ChEMBL ID CHEMBL2425081
Phase Preclinical
Structure Type MOL
InChI Key JFUBTJMMAHQVJI-SGIREYDYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

320.3
MW (Da)
1.86
ALogP
4
HBA
2
HBD
67.2
PSA (Ų)
0.89
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 C16H18F2N4O
MW 320.34
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.78

Activity Summary

IC50 3 meas. best 4.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 4.88 4.88 13100.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.81 4.81 15400.0 1
Prolyl endopeptidase FAP
CHEMBL4683
IC50 4.29 4.29 51000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 13100.0 nM 4.88 Inhibition of human DPP4 23972441
Dipeptidyl peptidase 2 IC50 = 15400.0 nM 4.81 Inhibition of QPP (unknown origin) 23972441
Prolyl endopeptidase FAP IC50 = 51000.0 nM 4.29 Inhibition of human FAP 23972441

Literature References

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

Data from ChEMBL 36 via Core Engine