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Compound Detail

CHEMBL106061

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CN1CCOCCn2cc(c3ccccc32)C2=C(C(=O)NC2=O)c2cn(c3ccccc23)CCOCC1

Basic Information

ChEMBL ID CHEMBL106061
Phase Preclinical
Structure Type MOL
InChI Key JISUVVYQUNDVBH-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
3.14
ALogP
7
HBA
1
HBD
77.7
PSA (Ų)
0.38
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30N4O4
MW 498.58
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.26

Activity Summary

IC50 5 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C beta type
CHEMBL3045
IC50 7.39 7.36 41.0 2
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 7.15 7.15 71.0 1
Protein kinase C epsilon type
CHEMBL3582
IC50 6.6 6.6 250.0 1
Protein kinase C alpha type
CHEMBL299
IC50 6.52 6.52 300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C beta type 2
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C alpha type 1
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C gamma type 1
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C delta type 1
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C epsilon type 1
12941331 10.1016/s0960-894x(03)00644-9 Protein kinase C zeta type 1
12941331 10.1016/s0960-894x(03)00644-9 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine