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Compound Detail

CHEMBL77002

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COc1cc(OC)cc(-c2cc3[nH]ccnc-3n2)c1

Basic Information

ChEMBL ID CHEMBL77002
Phase Preclinical
Structure Type MOL
InChI Key KVKNGELEWHXDPA-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

255.3
MW (Da)
2.59
ALogP
4
HBA
1
HBD
60.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H13N3O2
MW 255.28
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.98

Activity Summary

IC50 4 meas. best 4.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3
CHEMBL2095188
IC50 4.22 4.22 60256.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 4.22 4.22 60000.0 2
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12519061 10.1021/jm020319p Cyclin-dependent kinase 1/cyclin B 1
12519061 10.1021/jm020319p Cyclin-dependent kinase 5/CDK5 activator 1 1
12519061 10.1021/jm020319p Glycogen synthase kinase-3 beta 1
15603961 10.1016/j.bmcl.2004.10.060 Glycogen synthase kinase-3 1
18929433 10.1016/j.ejmech.2008.08.012 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine