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Compound Detail

CHEMBL4529301

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Cc1cccc(-c2nnc3ccc(N4CCN(C(=O)c5ccccc5)CC4)nn23)c1

Basic Information

ChEMBL ID CHEMBL4529301
Phase Preclinical
Structure Type MOL
InChI Key UPYOZLWVEBOJPB-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

398.5
MW (Da)
3.06
ALogP
6
HBA
0
HBD
66.6
PSA (Ų)
0.53
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N6O
MW 398.47
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -2.38

Activity Summary

IC50 2 meas. best 8.82
Ki 1 meas. best 7.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
INS1(832/13)
CHEMBL4483248
IC50 8.82 8.82 1.5 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.65 8.65 2.2 1
Dipeptidyl peptidase 4
CHEMBL284
Ki 7.88 7.88 13.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31812034 10.1016/j.ejmech.2019.111912 INS1(832/13) 5
31812034 10.1016/j.ejmech.2019.111912 Dipeptidyl peptidase 4 3
31812034 10.1016/j.ejmech.2019.111912 No relevant target 2

Data from ChEMBL 36 via Core Engine