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Compound Detail

CHEMBL400068

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N[C@@H](CC(=O)N1CCn2nc(C(F)(F)F)nc2[C@H]1Cn1cncn1)Cc1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL400068
Phase Preclinical
Structure Type MOL
InChI Key ALGBOHOONNECEK-IAQYHMDHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

488.4
MW (Da)
1.85
ALogP
8
HBA
1
HBD
107.8
PSA (Ų)
0.42
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 C19H18F6N8O
MW 488.40
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.41

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.7 8.7 2.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 2.0 nM 8.7 Inhibition of DPP4 17827003
Dipeptidyl peptidase 2 IC50 = 22000.0 nM 4.66 Inhibition of QPP 17827003

Literature References

PubMed DOI Target Context # Activities
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 4 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 8 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 9 1
17827003 10.1016/j.bmcl.2007.07.100 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine