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Compound Detail

CHEMBL475169

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CC(C)(CC(=O)N1CCn2nc(C(F)(F)F)nc2C1)[C@H](N)C(=O)N1CCC[C@H]1C#N.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL475169
Phase Preclinical
Structure Type MOL
InChI Key RUUMSRLPLPRFKH-YECZQDJWSA-N
Parent Compound CHEMBL1186714
Active Moiety CHEMBL1186714
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

427.4
MW (Da)
0.90
ALogP
7
HBA
1
HBD
121.1
PSA (Ų)
0.76
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 C20H25F6N7O4
MW 541.45
Aromatic Rings 1
Heavy Atoms 30
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.51 7.51 31.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.21 5.21 6200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 31.0 nM 7.51 Inhibition of DPP4 19269819
Dipeptidyl peptidase 8 IC50 = 6200.0 nM 5.21 Inhibition of DPP8 19269819

Literature References

PubMed DOI Target Context # Activities
19269819 10.1016/j.bmcl.2009.02.061 Unchecked 2
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 4 1
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 8 1
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine