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Compound Detail

CHEMBL1744354

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N#Cc1ccc(NCCNCC(=O)N2C[C@@H](F)C[C@H]2C#N)nc1.O=C(O)/C=C\C(=O)O

Basic Information

ChEMBL ID CHEMBL1744354
Phase Preclinical
Structure Type MOL
InChI Key JRBWXQVZEQZDJB-VNNDMRDYSA-N
Parent Compound CHEMBL488207
Active Moiety CHEMBL488207
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

316.3
MW (Da)
0.42
ALogP
6
HBA
2
HBD
104.8
PSA (Ų)
0.74
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21FN6O5
MW 432.41
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -1.46

Activity Summary

IC50 1 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.96 8.96 1.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 1.1 nM 8.96 Inhibition of DPP4 in human plasma by fluorescence assay 18243000

Literature References

PubMed DOI Target Context # Activities
18243000 10.1016/j.bmc.2008.01.016 Plasma 4
18243000 10.1016/j.bmc.2008.01.016 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine