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Compound Detail

CHEMBL217040

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C#C[C@H]1CC[C@@H](C#N)N1C(=O)CN[C@H]1CC[C@H](Oc2ccc(C#N)cn2)CC1

Basic Information

ChEMBL ID CHEMBL217040
Phase Preclinical
Structure Type MOL
InChI Key CBFPTXDGNGGMLX-VJANTYMQSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

377.4
MW (Da)
1.75
ALogP
6
HBA
1
HBD
102.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N5O2
MW 377.45
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.89

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
Ki 8.3 8.3 5.0 1
Dipeptidyl peptidase 9
CHEMBL4793
Ki 4.64 4.64 23000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 Ki = 5.0 nM 8.3 Inhibition of human DPP4 expressed in Caco-2 cells 17034148
Dipeptidyl peptidase 9 Ki = 23000.0 nM 4.64 Inhibition of DPP9 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