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Compound Detail

CHEMBL8179

WIN-57294
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Cc1cc(-c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)cc(C)n1

Basic Information

ChEMBL ID CHEMBL8179
Name WIN-57294
Phase Preclinical
Structure Type MOL
InChI Key WHXJSJBKDGZVDA-UHFFFAOYSA-N
2
Targets
8
Activities
2
Assay Types
0
PK Parameters
17
Publications
0
Known Names

Molecular Properties

370.4
MW (Da)
3.99
ALogP
4
HBA
1
HBD
72.2
PSA (Ų)
0.76
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 C20H16F2N2O3
MW 370.36
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.51

Activity Summary

EC50 5 meas. best 5.12
IC50 3 meas. best 4.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase II
CHEMBL2094255
EC50 5.12 5.12 7600.0 5
P388
CHEMBL389
IC50 4.54 4.54 29000.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00160-U Mus musculus 2
- 10.1016/0960-894X(95)00044-T Mus musculus 2
- 10.1016/0960-894X(95)00044-T DNA topoisomerase II 1
- 10.1016/0960-894X(95)00043-S DNA topoisomerase II 1
12459024 10.1021/jm010057b DNA topoisomerase II 1
- 10.1016/0960-894X(95)00160-U P388 1
- 10.1016/0960-894X(95)00160-U DNA topoisomerase II 1
- 10.1016/0960-894X(95)00044-T DNA topoisomerase 2-beta 1
- 10.1016/0960-894X(95)00044-T P388 1
7629792 10.1021/jm00014a005 Staphylococcus aureus 1
8410993 10.1021/jm00071a010 P388 1
8410993 10.1021/jm00071a010 DNA topoisomerase II 1
7629792 10.1021/jm00014a005 Bacteroides fragilis 1
7629792 10.1021/jm00014a005 Pseudomonas aeruginosa 1
7629792 10.1021/jm00014a005 Escherichia coli 1
7629792 10.1021/jm00014a005 Streptococcus pyogenes 1
7629792 10.1021/jm00014a005 Enterococcus faecalis 1

Data from ChEMBL 36 via Core Engine