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Compound Detail

CHEMBL400752

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N[C@@H](CC(=O)N1CCn2nc(C(F)(F)F)nc2[C@H]1CC1CC1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL400752
Phase Preclinical
Structure Type MOL
InChI Key UBCLRDQHUNDJBO-MLGOLLRUSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

461.4
MW (Da)
3.36
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21F6N5O
MW 461.41
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.15 8.15 7.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.13 5.13 7400.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.27 4.27 54000.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.15 4.15 71000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 7.0 nM 8.15 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 7400.0 nM 5.13 Inhibition of QPP 17827003
Dipeptidyl peptidase 9 IC50 = 54000.0 nM 4.27 Inhibition of DPP9 17827003
Dipeptidyl peptidase 8 IC50 = 71000.0 nM 4.15 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 2 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 8 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 9 1

Data from ChEMBL 36 via Core Engine