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Compound Detail

CHEMBL520921

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N#Cc1c(F)cc(F)cc1N1C[C@@H]2[C@H](C1)[C@H]2NCC(=O)N1C[C@@H](F)C[C@H]1C#N

Basic Information

ChEMBL ID CHEMBL520921
Phase Preclinical
Structure Type MOL
InChI Key OOUJXBPKJBAPMD-NEYKFGMSSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

389.4
MW (Da)
1.32
ALogP
5
HBA
1
HBD
83.2
PSA (Ų)
0.84
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 C19H18F3N5O
MW 389.38
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.86

Activity Summary

IC50 5 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.2 6.2 630.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.71 5.71 1960.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.69 5.69 2050.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.41 5.41 3900.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 5.06 5.06 8700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 630.0 nM 6.2 Inhibition of human plasma DPP4 18602260
Dipeptidyl peptidase 9 IC50 = 1960.0 nM 5.71 Inhibition of DPP9 18602260
Dipeptidyl peptidase 8 IC50 = 2050.0 nM 5.69 Inhibition of DPP8 18602260
Dipeptidyl peptidase 2 IC50 = 3900.0 nM 5.41 Inhibition of DPP2 18602260
Prolyl endopeptidase IC50 = 8700.0 nM 5.06 Inhibition of PPCE 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