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Compound Detail

CHEMBL217252

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C#C[C@H]1CC[C@@H](C#N)N1C(=O)[C@@H](N)C1CCCC1

Basic Information

ChEMBL ID CHEMBL217252
Phase Preclinical
Structure Type MOL
InChI Key WLGYZHSSENEZRE-AVGNSLFASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

245.3
MW (Da)
1.02
ALogP
3
HBA
1
HBD
70.1
PSA (Ų)
0.74
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H19N3O
MW 245.33
Aromatic Rings 0
Heavy Atoms 18
NP-Likeness 0.20

Activity Summary

Ki 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
Ki 8.1 8.1 8.0 1
Dipeptidyl peptidase 8
CHEMBL4657
Ki 4.75 4.75 17700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 Ki = 8.0 nM 8.1 Inhibition of human DPP4 expressed in Caco-2 cells 17034148
Dipeptidyl peptidase 8 Ki = 17700.0 nM 4.75 Inhibition of DPP8 17034148

Literature References

PubMed DOI Target Context # Activities
17034148 10.1021/jm060777o Dipeptidyl peptidase 4 1
17034148 10.1021/jm060777o Dipeptidyl peptidase 8 1
17034148 10.1021/jm060777o Dipeptidyl peptidase 9 1

Data from ChEMBL 36 via Core Engine