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Compound Detail

CHEMBL218306

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C[C@H](c1n[nH]c(-c2ccc(Cl)cc2Cl)n1)[C@H](N)C(=O)N1CCCC1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL218306
Phase Preclinical
Structure Type MOL
InChI Key MWJOBRNZTGWNNK-NAWISMDQSA-N
Parent Compound CHEMBL1182194
Active Moiety CHEMBL1182194
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

368.3
MW (Da)
2.83
ALogP
4
HBA
2
HBD
87.9
PSA (Ų)
0.87
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 C18H20Cl2F3N5O3
MW 482.29
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.42

Activity Summary

IC50 2 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 5.52 5.52 3050.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.27 5.27 5410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 3050.0 nM 5.52 Inhibition of DPP4 16919457
Dipeptidyl peptidase 2 IC50 = 5410.0 nM 5.27 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