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Compound Detail

CHEMBL1683096

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CS(=O)(=O)N(Cc1ccccc1)[C@H]1CC[C@H]([C@H](N)Cc2cc(F)ccc2F)CC1

Basic Information

ChEMBL ID CHEMBL1683096
Phase Preclinical
Structure Type MOL
InChI Key GJFPOKRDCKMHQY-NQSCKRDGSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

422.5
MW (Da)
3.86
ALogP
3
HBA
1
HBD
63.4
PSA (Ų)
0.74
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28F2N2O2S
MW 422.54
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.36

Activity Summary

IC50 3 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 5.89 5.89 1300.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.96 4.96 11000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.26 4.26 55000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 1300.0 nM 5.89 Inhibition of DPP4 21320777
Dipeptidyl peptidase 2 IC50 = 11000.0 nM 4.96 Inhibition of QPP 21320777
Dipeptidyl peptidase 9 IC50 = 55000.0 nM 4.26 Inhibition of DPP9 21320777

Literature References

PubMed DOI Target Context # Activities
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 4 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 2 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 8 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 9 1
21320777 10.1016/j.bmcl.2010.12.060 Prolyl endopeptidase FAP 1

Data from ChEMBL 36 via Core Engine