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Compound Detail

CHEMBL479736

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N#C[C@@H]1C[C@H](F)CN1C(=O)CN[C@H]1[C@@H]2CN(c3ccc([N+](=O)[O-])cn3)C[C@@H]21

Basic Information

ChEMBL ID CHEMBL479736
Phase Preclinical
Structure Type MOL
InChI Key FKRMMWVMZKHKIJ-MXJLERKLSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
0.48
ALogP
7
HBA
1
HBD
115.4
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H19FN6O3
MW 374.38
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.31

Activity Summary

IC50 4 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.07 7.07 85.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.78 5.78 1667.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 5.07 5.07 8500.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.88 4.88 13050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 85.0 nM 7.07 Inhibition of human plasma DPP4 18602260
Dipeptidyl peptidase 8 IC50 = 1667.0 nM 5.78 Inhibition of DPP8 18602260
Prolyl endopeptidase IC50 = 8500.0 nM 5.07 Inhibition of PPCE 18602260
Dipeptidyl peptidase 2 IC50 = 13050.0 nM 4.88 Inhibition of DPP2 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