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Compound Detail

CHEMBL495545

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CN1CCN(c2ccc(Nc3nccc(-c4cnn5ncccc45)n3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL495545
Phase Preclinical
Structure Type MOL
InChI Key AUAUBVTWWCYNPP-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

386.5
MW (Da)
2.68
ALogP
8
HBA
1
HBD
74.5
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N8
MW 386.46
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.59

Activity Summary

IC50 4 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 7.92 7.92 12.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.0 7.0 100.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 6.7 6.7 200.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18835709 10.1016/j.bmcl.2008.09.069 Cyclin-dependent kinase 4 1
18835709 10.1016/j.bmcl.2008.09.069 Vascular endothelial growth factor receptor 2 1
18835709 10.1016/j.bmcl.2008.09.069 Glycogen synthase kinase-3 beta 1
18835709 10.1016/j.bmcl.2008.09.069 Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine