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Compound Detail

CHEMBL219371

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CC(C)C[C@H](c1nc(-c2ccc(S(C)(=O)=O)cc2Cl)no1)[C@H](N)C(=O)N1CC[C@H](F)C1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL219371
Phase Preclinical
Structure Type MOL
InChI Key MMPHCTQPQORTIR-JPZWBZILSA-N
Parent Compound CHEMBL1182199
Active Moiety CHEMBL1182199
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.0
MW (Da)
2.82
ALogP
7
HBA
1
HBD
119.4
PSA (Ų)
0.66
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 C22H27ClF4N4O6S
MW 586.99
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.56

Activity Summary

IC50 2 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.89 7.89 13.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.43 5.43 3700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 13.0 nM 7.89 Inhibition of DPP4 16919457
Dipeptidyl peptidase 2 IC50 = 3700.0 nM 5.43 Inhibition of QPP 16919457

Literature References

PubMed DOI Target Context # Activities
16919457 10.1016/j.bmcl.2006.07.061 Dipeptidyl peptidase 4 1
16919457 10.1016/j.bmcl.2006.07.061 Dipeptidyl peptidase 2 1
16919457 10.1016/j.bmcl.2006.07.061 Dipeptidyl peptidase 9 1
16919457 10.1016/j.bmcl.2006.07.061 Dipeptidyl peptidase 8 1

Data from ChEMBL 36 via Core Engine