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Compound Detail

CHEMBL201424

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CC(C)(CC(=O)N1CCc2ccccc2C1)NCC(=O)N1CCC[C@H]1C#N

Basic Information

ChEMBL ID CHEMBL201424
Phase Preclinical
Structure Type MOL
InChI Key VKFKZRVCMJZWMP-SFHVURJKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
1.84
ALogP
4
HBA
1
HBD
76.4
PSA (Ų)
0.86
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28N4O2
MW 368.48
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.31 7.31 49.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.47 4.47 34201.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 49.0 nM 7.31 Inhibitory activity against DPP4 16392822
Dipeptidyl peptidase 2 IC50 = 34201.0 nM 4.47 Inhibitory activity against DPP2 16392822

Literature References

PubMed DOI Target Context # Activities
16392822 10.1021/jm0507781 Dipeptidyl peptidase 4 3
16392822 10.1021/jm0507781 No relevant target 2
16392822 10.1021/jm0507781 Dipeptidyl peptidase 8 1
16392822 10.1021/jm0507781 Dipeptidyl peptidase 2 1
16392822 10.1021/jm0507781 Unchecked 1

Data from ChEMBL 36 via Core Engine