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Compound Detail

CHEMBL428339

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Cc1cc(-c2c(F)cc3c(=O)c(Cc4c(O)cc(O)cc4O)cn(C4CC4)c3c2F)cc(C)n1

Basic Information

ChEMBL ID CHEMBL428339
Phase Preclinical
Structure Type MOL
InChI Key RFDGFRCCZHJVEL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

464.5
MW (Da)
5.00
ALogP
6
HBA
3
HBD
95.6
PSA (Ų)
0.40
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H22F2N2O4
MW 464.47
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.04

Activity Summary

EC50 1 meas. best 7.01
IC50 1 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase II
CHEMBL2094255
EC50 7.01 7.01 98.0 1
P388
CHEMBL389
IC50 6.33 6.33 470.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase II EC50 = 98.0 nM 7.01 Inhibitory activity against HeLa cell Topoisomerase II -
P388 IC50 = 470.0 nM 6.33 In vitro cytotoxicity against P388 mouse leukemia cells -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00160-U DNA topoisomerase II 1
- 10.1016/0960-894X(95)00160-U P388 1

Data from ChEMBL 36 via Core Engine