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Compound Detail

CHEMBL489833

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Cn1cc(C2=C(c3coc4cc(CO)ccc34)C(=O)NC2=O)c2cc(Br)ccc21

Basic Information

ChEMBL ID CHEMBL489833
Phase Preclinical
Structure Type MOL
InChI Key GAVPKFXPGFHFSY-UHFFFAOYSA-N
8
Targets
10
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

451.3
MW (Da)
3.75
ALogP
5
HBA
2
HBD
84.5
PSA (Ų)
0.47
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 C22H15BrN2O4
MW 451.28
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness 0.08

Activity Summary

IC50 10 meas. best 9.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 9.29 9.29 0.5 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.47 6.365 337.0 2
CDK6/cyclin D3
CHEMBL2111448
IC50 6.29 6.29 510.0 1
Cyclin-dependent kinase 1/cyclin B1
CHEMBL1907602
IC50 6.03 6.03 930.0 1
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 5.97 5.97 1080.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.95 5.945 1130.0 2
CDK9/cyclin T1
CHEMBL2111389
IC50 5.91 5.91 1220.0 1
Cyclin-dependent kinase 3
CHEMBL4442
IC50 5.91 5.91 1220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19338355 10.1021/jm801317h Unchecked 9
19338355 10.1021/jm801317h Cyclin-dependent kinase 2 2
19338355 10.1021/jm801317h Cyclin-dependent kinase 5/CDK5 activator 1 2
19338355 10.1021/jm801317h Glycogen synthase kinase-3 beta 1
19338355 10.1021/jm801317h Cyclin-dependent kinase 1/cyclin B1 1
19338355 10.1021/jm801317h Cyclin-dependent kinase 3 1
19338355 10.1021/jm801317h Cyclin-dependent kinase 4/cyclin D1 1
19338355 10.1021/jm801317h CDK6/cyclin D3 1
19338355 10.1021/jm801317h CDK9/cyclin T1 1

Data from ChEMBL 36 via Core Engine