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Compound Detail

CHEMBL216835

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C[C@H](c1nc(-c2ccc(S(C)(=O)=O)cc2Cl)no1)[C@H](N)C(=O)N1CCCC1

Basic Information

ChEMBL ID CHEMBL216835
Phase Preclinical
Structure Type MOL
InChI Key OQFYSOSOPKUSCH-HZMBPMFUSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

412.9
MW (Da)
1.85
ALogP
7
HBA
1
HBD
119.4
PSA (Ų)
0.80
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 C17H21ClN4O4S
MW 412.90
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.77

Activity Summary

IC50 2 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.77 7.77 17.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.19 5.19 6400.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 6.0 mL.min-1.kg-1 Rattus norvegicus
F 27.0 % Rattus norvegicus
T1/2 0.82 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 17.0 nM 7.77 Inhibition of DPP4 16919457
Dipeptidyl peptidase 2 IC50 = 6400.0 nM 5.19 Inhibition of QPP 16919457

Literature References

PubMed DOI Target Context # Activities
16919457 10.1016/j.bmcl.2006.07.061 Rattus norvegicus 3
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
16919457 10.1016/j.bmcl.2006.07.061 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine