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Compound Detail

CHEMBL609040

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O=C1Nc2cc3c(O)cccc3c3c4c(cc1c23)OCO4

Basic Information

ChEMBL ID CHEMBL609040
Phase Preclinical
Structure Type MOL
InChI Key OVACCXPNQSWBBB-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

279.2
MW (Da)
2.99
ALogP
4
HBA
2
HBD
67.8
PSA (Ų)
0.62
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C16H9NO4
MW 279.25
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness 1.44

Activity Summary

IC50 5 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.46 7.46 35.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.67 6.67 214.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 5.85 5.85 1420.0 1
Aurora kinase A
CHEMBL4722
IC50 5.67 5.67 2140.0 1
Unchecked
CHEMBL612545
IC50 4.45 4.45 35335.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 35.0 nM 7.46 Inhibition of CDK2 20097066
Cyclin-dependent kinase 1 IC50 = 214.0 nM 6.67 Inhibition of CDC2 20097066
Cyclin-dependent kinase 4 IC50 = 1420.0 nM 5.85 Inhibition of CDK4 20097066
Aurora kinase A IC50 = 2140.0 nM 5.67 Inhibition of AUR2 20097066
Unchecked IC50 = 35335.0 nM 4.45 Inhibition of MAPK 20097066

Literature References

PubMed DOI Target Context # Activities
20097066 10.1016/j.bmcl.2010.01.007 Cyclin-dependent kinase 2 2
20097066 10.1016/j.bmcl.2010.01.007 Cyclin-dependent kinase 1 1
20097066 10.1016/j.bmcl.2010.01.007 Cyclin-dependent kinase 4 1
20097066 10.1016/j.bmcl.2010.01.007 Aurora kinase A 1
20097066 10.1016/j.bmcl.2010.01.007 Unchecked 1

Data from ChEMBL 36 via Core Engine