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Compound Detail

CHEMBL401304

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N[C@@H](CC(=O)N1CCn2nc(C(F)(F)F)nc2[C@H]1Cc1ccc(F)cc1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL401304
Phase Preclinical
Structure Type MOL
InChI Key ILWOOGUHZKNTQQ-DNVCBOLYSA-N
4
Targets
4
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

515.4
MW (Da)
3.94
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.40
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20F7N5O
MW 515.43
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.4 8.4 4.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.6 4.6 25000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.57 4.57 27000.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.22 4.22 60000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 0.146 uM.hr.Kg/mg Rattus norvegicus
CL 76.0 mL.min-1.kg-1 Rattus norvegicus
F 32.0 % Rattus norvegicus
T1/2 2.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 4.0 nM 8.4 Inhibition of DPP4 17827003
Dipeptidyl peptidase 8 IC50 = 25000.0 nM 4.6 Inhibition of DPP8 17827003
Dipeptidyl peptidase 9 IC50 = 27000.0 nM 4.57 Inhibition of DPP9 17827003
Dipeptidyl peptidase 2 IC50 = 60000.0 nM 4.22 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 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