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Compound Detail

CHEMBL481669

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N#Cc1ccc(N2C[C@@H]3[C@H](C2)[C@H]3NCC(=O)N2C[C@@H](F)C[C@H]2C#N)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL481669
Phase Preclinical
Structure Type MOL
InChI Key YJMLPSBGVRXCPM-LADRPBIPSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

387.9
MW (Da)
1.70
ALogP
5
HBA
1
HBD
83.2
PSA (Ų)
0.85
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19ClFN5O
MW 387.85
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.02

Activity Summary

IC50 5 meas. best 7.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 9
CHEMBL4793
IC50 7.18 7.18 66.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.02 7.02 95.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 6.41 6.41 392.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.4 6.4 399.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 9 IC50 = 66.0 nM 7.18 Inhibition of DPP9 18602260
Dipeptidyl peptidase 4 IC50 = 95.0 nM 7.02 Inhibition of human plasma DPP4 18602260
Prolyl endopeptidase IC50 = 392.0 nM 6.41 Inhibition of PPCE 18602260
Dipeptidyl peptidase 8 IC50 = 399.0 nM 6.4 Inhibition of DPP8 18602260
Dipeptidyl peptidase 2 IC50 = 1000.0 nM 6.0 Inhibition of DPP2 18602260

Literature References

PubMed DOI Target Context # Activities
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 4 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 2 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 8 1
18602260 10.1016/j.bmcl.2008.05.101 Dipeptidyl peptidase 9 1
18602260 10.1016/j.bmcl.2008.05.101 Prolyl endopeptidase 1

Data from ChEMBL 36 via Core Engine