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Compound Detail

CHEMBL224666

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COc1ccc(C(=O)Nc2c(O)cc(O)c3c(=O)cc(-c4ccccc4Cl)oc23)cc1

Basic Information

ChEMBL ID CHEMBL224666
Phase Preclinical
Structure Type MOL
InChI Key HDOFRSOUPSLNLW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

437.8
MW (Da)
4.79
ALogP
6
HBA
3
HBD
109.0
PSA (Ų)
0.31
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 C23H16ClNO6
MW 437.84
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.02

Activity Summary

IC50 2 meas. best 4.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 4.89 4.89 13000.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 4.27 4.27 54000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 13000.0 nM 4.89 Antiproliferative activity against MCF7 cells 17123821
Cyclin-dependent kinase 2/cyclin A IC50 = 54000.0 nM 4.27 Inhibition of CDK2/Cyclin A 17123821

Literature References

PubMed DOI Target Context # Activities
17123821 10.1016/j.bmc.2006.10.063 NON-PROTEIN TARGET 1
17123821 10.1016/j.bmc.2006.10.063 MCF7 1
17123821 10.1016/j.bmc.2006.10.063 Cyclin-dependent kinase 2/cyclin A 1

Data from ChEMBL 36 via Core Engine