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Compound Detail

CHEMBL4530328

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O=c1nc(NC[C@@H](O)CN2CCN(c3nccc4ccc(F)cc34)CC2)c2ccccc2o1

Basic Information

ChEMBL ID CHEMBL4530328
Phase Preclinical
Structure Type MOL
InChI Key ILSQZDCVJPCWKM-GOSISDBHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
2.47
ALogP
8
HBA
2
HBD
94.7
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24FN5O3
MW 449.49
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.18

Activity Summary

IC50 4 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA topoisomerase 4 subunit A
CHEMBL4088
IC50 6.52 6.52 300.0 1
DNA topoisomerase 4 subunit A
CHEMBL1895
IC50 6.4 6.4 400.0 1
DNA gyrase subunit A
CHEMBL2424506
IC50 6.22 6.22 600.0 1
DNA gyrase subunit A
CHEMBL1858
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31276392 10.1021/acs.jmedchem.9b00394 DNA topoisomerase 4 subunit A 2
31276392 10.1021/acs.jmedchem.9b00394 DNA gyrase subunit A 2
31276392 10.1021/acs.jmedchem.9b00394 Staphylococcus aureus 2
31276392 10.1021/acs.jmedchem.9b00394 Escherichia coli 1
31276392 10.1021/acs.jmedchem.9b00394 Pseudomonas aeruginosa 1

Data from ChEMBL 36 via Core Engine