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Compound Detail

CHEMBL527647

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O=C([C@@H]1C[C@H](Nc2cccc3ccccc23)CN1)N1Cc2ccccc2C1

Basic Information

ChEMBL ID CHEMBL527647
Phase Preclinical
Structure Type MOL
InChI Key WARLRLQWEAJUET-UGKGYDQZSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

357.5
MW (Da)
3.52
ALogP
3
HBA
2
HBD
44.4
PSA (Ų)
0.75
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 C23H23N3O
MW 357.46
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.64

Activity Summary

IC50 4 meas. best 6.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.15 6.15 710.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 6.07 6.07 860.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 5.3 5.3 4970.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.39 4.39 41000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 8 IC50 = 710.0 nM 6.15 Inhibition of DPP8 18556198
Dipeptidyl peptidase 2 IC50 = 860.0 nM 6.07 Inhibition of DPP2 18556198
Dipeptidyl peptidase 4 IC50 = 4970.0 nM 5.3 Inhibition of DPP4 18556198
Dipeptidyl peptidase 9 IC50 = 41000.0 nM 4.39 Inhibition of DPP9 18556198

Literature References

PubMed DOI Target Context # Activities
18556198 10.1016/j.bmcl.2008.05.079 Dipeptidyl peptidase 8 1
18556198 10.1016/j.bmcl.2008.05.079 Dipeptidyl peptidase 9 1
18556198 10.1016/j.bmcl.2008.05.079 Dipeptidyl peptidase 4 1
18556198 10.1016/j.bmcl.2008.05.079 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine