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Compound Detail

CHEMBL1651767

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Cc1csc2c(=O)n(Cc3ccccc3C#N)c(N3CCC[C@@H](N)C3)nc12

Basic Information

ChEMBL ID CHEMBL1651767
Phase Preclinical
Structure Type MOL
InChI Key KATIUIKHAYYOMJ-MRXNPFEDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

379.5
MW (Da)
2.61
ALogP
7
HBA
1
HBD
87.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21N5OS
MW 379.49
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.81

Activity Summary

IC50 1 meas. best 8.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.76 8.76 1.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 1.72 nM 8.76 Inhibition of DPP4 after 20 mins by fluorescence assay 21106276

Literature References

PubMed DOI Target Context # Activities
21106276 10.1016/j.ejmech.2010.10.016 Dipeptidyl peptidase 4 1
21106276 10.1016/j.ejmech.2010.10.016 Dipeptidyl peptidase 8 1
21106276 10.1016/j.ejmech.2010.10.016 Dipeptidyl peptidase 9 1
21106276 10.1016/j.ejmech.2010.10.016 Voltage-gated inwardly rectifying potassium channel KCNH2 1
22475866 10.1016/j.ejmech.2012.03.015 Liver microsomes 1

Data from ChEMBL 36 via Core Engine