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Compound Detail

CHEMBL399499

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

Basic Information

ChEMBL ID CHEMBL399499
Phase Preclinical
Structure Type MOL
InChI Key YLGVHOFWOIUHJN-SECBINFHSA-N
3
Targets
3
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

407.3
MW (Da)
2.02
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15F6N5O
MW 407.32
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.47

Activity Summary

IC50 3 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.23 7.23 59.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.27 4.27 54000.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.21 4.21 62000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1.143 uM.hr.Kg/mg Rattus norvegicus
CL 60.0 mL.min-1.kg-1 Rattus norvegicus
F 100.0 % Rattus norvegicus
T1/2 3.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 59.0 nM 7.23 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 54000.0 nM 4.27 Inhibition of QPP 17827003
Dipeptidyl peptidase 8 IC50 = 62000.0 nM 4.21 Inhibition of DPP8 17827003

Literature References

PubMed DOI Target Context # Activities
17827003 10.1016/j.bmcl.2007.07.100 Rattus norvegicus 4
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