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Compound Detail

CHEMBL224038

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O=C(Nc1c(O)cc(O)c2c(=O)cc(-c3ccccc3Cl)oc12)c1ccccc1

Basic Information

ChEMBL ID CHEMBL224038
Phase Preclinical
Structure Type MOL
InChI Key JFCDKCMLPYSMPY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.8
MW (Da)
4.78
ALogP
5
HBA
3
HBD
99.8
PSA (Ų)
0.34
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 C22H14ClNO5
MW 407.81
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness 0.03

Activity Summary

IC50 2 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 5.07 5.07 8500.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 4.04 4.04 91000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 8500.0 nM 5.07 Antiproliferative activity against MCF7 cells 17123821
Cyclin-dependent kinase 2/cyclin A IC50 = 91000.0 nM 4.04 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