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Compound Detail

CHEMBL452998

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N#Cc1cccnc1N1C[C@@H]2[C@H](C1)[C@H]2NCC(=O)N1C[C@@H](F)C[C@H]1C#N

Basic Information

ChEMBL ID CHEMBL452998
Phase Preclinical
Structure Type MOL
InChI Key AEXGTOIVMLLERR-NBFUAULTSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

354.4
MW (Da)
0.44
ALogP
6
HBA
1
HBD
96.0
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 C18H19FN6O
MW 354.39
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -0.99

Activity Summary

IC50 5 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.04 7.04 91.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.87 5.87 1340.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.14 5.14 7300.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 4.93 4.93 11790.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.79 4.79 16100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 91.0 nM 7.04 Inhibition of human plasma DPP4 18602260
Dipeptidyl peptidase 2 IC50 = 1340.0 nM 5.87 Inhibition of DPP2 18602260
Dipeptidyl peptidase 9 IC50 = 7300.0 nM 5.14 Inhibition of DPP9 18602260
Prolyl endopeptidase IC50 = 11790.0 nM 4.93 Inhibition of PPCE 18602260
Dipeptidyl peptidase 8 IC50 = 16100.0 nM 4.79 Inhibition of DPP8 18602260

Literature References

PubMed DOI Target Context # Activities
18602260 10.1016/j.bmcl.2008.05.101 Unchecked 3
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
18602260 10.1016/j.bmcl.2008.05.101 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine