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Compound Detail

CHEMBL224029

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Cc1ccc(C(=O)Nc2c(O)cc(O)c3c(=O)cc(-c4ccccc4Cl)oc23)cc1

Basic Information

ChEMBL ID CHEMBL224029
Phase Preclinical
Structure Type MOL
InChI Key GBBQBUWBDUTFCA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

421.8
MW (Da)
5.09
ALogP
5
HBA
3
HBD
99.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H16ClNO5
MW 421.84
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.11

Activity Summary

IC50 2 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 5.01 5.01 9700.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 4.05 4.05 90000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 9700.0 nM 5.01 Antiproliferative activity against MCF7 cells 17123821
Cyclin-dependent kinase 2/cyclin A IC50 = 90000.0 nM 4.05 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