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Compound Detail

CHEMBL250147

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N[C@@H](CC(=O)N1CCn2nc(C(F)(F)F)nc2C1Cn1ccnc1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL250147
Phase Preclinical
Structure Type MOL
InChI Key CKIFCELIDODOGV-ZGTOLYCTSA-N
3
Targets
3
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

487.4
MW (Da)
2.45
ALogP
7
HBA
1
HBD
94.9
PSA (Ų)
0.43
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 C20H19F6N7O
MW 487.41
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.36

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.7 8.7 2.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.58 4.58 26000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.57 4.57 27000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 0.027 uM.hr.Kg/mg Rattus norvegicus
CL 97.0 mL.min-1.kg-1 Rattus norvegicus
F 7.1 % Rattus norvegicus
T1/2 9.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 2.0 nM 8.7 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 26000.0 nM 4.58 Inhibition of QPP 17827003
Dipeptidyl peptidase 9 IC50 = 27000.0 nM 4.57 Inhibition of DPP9 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 2 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 9 1

Data from ChEMBL 36 via Core Engine