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Compound Detail

CHEMBL427219

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O=C([C@@H]1CN[C@H](C(=O)N2CCC(F)(F)C2)C1)N1Cc2ccccc2C1

Basic Information

ChEMBL ID CHEMBL427219
Phase Preclinical
Structure Type MOL
InChI Key VJUQFPMKSWQOBY-GJZGRUSLSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

349.4
MW (Da)
1.37
ALogP
3
HBA
1
HBD
52.6
PSA (Ų)
0.88
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21F2N3O2
MW 349.38
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness -0.51

Activity Summary

IC50 3 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.89 6.89 129.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.72 4.72 19250.0 1
Prolyl endopeptidase FAP
CHEMBL4683
IC50 4.71 4.71 19478.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 129.0 nM 6.89 Inhibition of DPP4 16581245
Dipeptidyl peptidase 2 IC50 = 19250.0 nM 4.72 Inhibition of DPP2 16581245
Prolyl endopeptidase FAP IC50 = 19478.0 nM 4.71 Inhibition of FAP 16581245

Literature References

PubMed DOI Target Context # Activities
16581245 10.1016/j.bmcl.2006.03.037 Dipeptidyl peptidase 4 1
16581245 10.1016/j.bmcl.2006.03.037 Dipeptidyl peptidase 8 1
16581245 10.1016/j.bmcl.2006.03.037 Dipeptidyl peptidase 2 1
16581245 10.1016/j.bmcl.2006.03.037 Prolyl endopeptidase FAP 1

Data from ChEMBL 36 via Core Engine