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Compound Detail

CHEMBL488492

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O=C([C@@H]1C[C@H](N(c2cccc3ccccc23)c2cccc3ccccc23)CN1)N1Cc2ccccc2C1

Basic Information

ChEMBL ID CHEMBL488492
Phase Preclinical
Structure Type MOL
InChI Key GGMAFYWNRMIHAN-FIBWVYCGSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

483.6
MW (Da)
6.40
ALogP
3
HBA
1
HBD
35.6
PSA (Ų)
0.32
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H29N3O
MW 483.62
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -0.42

Activity Summary

IC50 3 meas. best 5.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.77 5.77 1700.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.92 4.92 12000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.79 4.79 16100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 2 IC50 = 1700.0 nM 5.77 Inhibition of DPP2 18556198
Dipeptidyl peptidase 8 IC50 = 12000.0 nM 4.92 Inhibition of DPP8 18556198
Dipeptidyl peptidase 9 IC50 = 16100.0 nM 4.79 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