Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL494339

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
N#C[C@@H]1CCCN1C(=O)[C@@H](N)CCC(=O)N1CCc2nc(-c3ccc(F)cc3)sc2C1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL494339
Phase Preclinical
Structure Type MOL
InChI Key SDVRCAUGRBMIJI-QJHJCNPRSA-N
Parent Compound CHEMBL1187227
Active Moiety CHEMBL1187227
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

441.5
MW (Da)
2.46
ALogP
6
HBA
1
HBD
103.3
PSA (Ų)
0.77
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25F4N5O4S
MW 555.55
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.44

Activity Summary

IC50 4 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.4 7.4 40.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.0 6.0 1000.0 1
Unchecked
CHEMBL612545
IC50 5.64 5.64 2300.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 40.0 nM 7.4 Inhibition of DPP4 19269819
Dipeptidyl peptidase 8 IC50 = 1000.0 nM 6.0 Inhibition of DPP8 19269819
Unchecked IC50 = 2300.0 nM 5.64 Inhibition of FAP 19269819
Dipeptidyl peptidase 2 IC50 = 12000.0 nM 4.92 Inhibition of DPP2 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