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Compound Detail

CHEMBL441631

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Cc1cc(-c2c(F)c(F)c3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)cc(C)n1

Basic Information

ChEMBL ID CHEMBL441631
Phase Preclinical
Structure Type MOL
InChI Key QUYSIYPMTRHBAI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

388.4
MW (Da)
4.13
ALogP
4
HBA
1
HBD
72.2
PSA (Ų)
0.69
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 C20H15F3N2O3
MW 388.35
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.36

Activity Summary

EC50 1 meas. best 4.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase II
CHEMBL2094255
EC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA topoisomerase II EC50 = 13000.0 nM 4.89 Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleava... 8410993

Literature References

PubMed DOI Target Context # Activities
7629792 10.1021/jm00014a005 Staphylococcus aureus 1
7629792 10.1021/jm00014a005 Enterococcus faecalis 1
7629792 10.1021/jm00014a005 Streptococcus pyogenes 1
7629792 10.1021/jm00014a005 Escherichia coli 1
7629792 10.1021/jm00014a005 Pseudomonas aeruginosa 1
7629792 10.1021/jm00014a005 Bacteroides fragilis 1
8410993 10.1021/jm00071a010 DNA topoisomerase II 1

Data from ChEMBL 36 via Core Engine