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Compound Detail

CHEMBL186032

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CS(=O)(=O)Nc1cccc(NC(=O)CN2CCN(C[C@@H](N)Cc3ccccc3)C(Cc3ccccc3)C2)c1

Basic Information

ChEMBL ID CHEMBL186032
Phase Preclinical
Structure Type MOL
InChI Key FOJSXRONJUPKFM-ALLRNTDFSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

535.7
MW (Da)
2.80
ALogP
6
HBA
3
HBD
107.8
PSA (Ų)
0.35
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37N5O3S
MW 535.71
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.27

Activity Summary

IC50 2 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 4.96 4.96 11000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 11000.0 nM 4.96 Inhibitory concentration against Dipeptidylpeptidase IV 15324904
Dipeptidyl peptidase 4 IC50 = 11000.0 nM 4.96 Inhibition of DPP-4 (unknown origin) 37647598

Literature References

PubMed DOI Target Context # Activities
15324904 10.1016/j.bmcl.2004.06.065 Dipeptidyl peptidase 4 1
37647598 10.1021/acs.jmedchem.3c00412 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine