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Compound Detail

CHEMBL404210

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N[C@@H](CC(=O)N1CCn2nc(C(F)(F)F)nc2[C@@H]1C(O)C1CC1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL404210
Phase Preclinical
Structure Type MOL
InChI Key PWBSQBGRKYZZLO-JGCDQOMISA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

477.4
MW (Da)
2.33
ALogP
6
HBA
2
HBD
97.3
PSA (Ų)
0.49
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 C20H21F6N5O2
MW 477.41
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.83

Activity Summary

IC50 2 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.85 7.85 14.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.75 4.75 18000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 0.271 uM.hr.Kg/mg Rattus norvegicus
CL 97.0 mL.min-1.kg-1 Rattus norvegicus
F 63.0 % Rattus norvegicus
T1/2 3.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 14.0 nM 7.85 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 18000.0 nM 4.75 Inhibition of QPP 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 8 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

Data from ChEMBL 36 via Core Engine