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Compound Detail

CHEMBL372391

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CC(C)C(NC(=O)CCNCC(=O)N1CCC[C@H]1C#N)c1ccccc1

Basic Information

ChEMBL ID CHEMBL372391
Phase Preclinical
Structure Type MOL
InChI Key ALAZHGPNVAHHCA-DIMJTDRSSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

356.5
MW (Da)
1.99
ALogP
4
HBA
2
HBD
85.2
PSA (Ų)
0.70
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H28N4O2
MW 356.47
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -1.13

Activity Summary

IC50 3 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.11 6.11 784.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.89 4.89 12847.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.53 4.53 29315.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 784.0 nM 6.11 Inhibitory activity against DPP4 16392822
Dipeptidyl peptidase 8 IC50 = 12847.0 nM 4.89 Inhibitory activity against DPP8 16392822
Dipeptidyl peptidase 2 IC50 = 29315.0 nM 4.53 Inhibitory activity against DPP2 16392822

Literature References

PubMed DOI Target Context # Activities
16392822 10.1021/jm0507781 Dipeptidyl peptidase 4 1
16392822 10.1021/jm0507781 Dipeptidyl peptidase 8 1
16392822 10.1021/jm0507781 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine