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Compound Detail

CHEMBL401057

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N[C@@H](CC(=O)N1CCn2nc(-c3ccccc3)nc2C1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL401057
Phase Preclinical
Structure Type MOL
InChI Key VCTJXCYUKWWVIH-OAHLLOKOSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

415.4
MW (Da)
2.66
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.65
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 C21H20F3N5O
MW 415.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.36

Activity Summary

IC50 3 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.17 7.17 68.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.4 5.4 4000.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.36 4.36 44000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 68.0 nM 7.17 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 4000.0 nM 5.4 Inhibition of QPP 17827003
Dipeptidyl peptidase 8 IC50 = 44000.0 nM 4.36 Inhibition of DPP8 17827003

Literature References

PubMed DOI Target Context # Activities
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 4 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 9 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 2 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 8 1

Data from ChEMBL 36 via Core Engine