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Compound Detail

CHEMBL4091354

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COc1ccc2ncc(F)c([C@@H](O)CC[C@@H]3CCN(C4CC(c5cc(F)cc(F)c5F)C4)C[C@@H]3C(=O)O)c2c1

Basic Information

ChEMBL ID CHEMBL4091354
Phase Preclinical
Structure Type MOL
InChI Key KDTFKIILDVXBLZ-UYYXBMAPSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

546.6
MW (Da)
5.58
ALogP
5
HBA
2
HBD
82.9
PSA (Ų)
0.28
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30F4N2O4
MW 546.56
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.24

Activity Summary

IC50 2 meas. best 5.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.81 5.57 1560.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1560.0 nM 5.81 Inhibition of Staphylococcus aureus DNA gyrase 28610977
Unchecked IC50 = 4700.0 nM 5.33 Inhibition of Staphylococcus aureus DNA topoisomerase 4 28610977

Literature References

PubMed DOI Target Context # Activities
28610977 10.1016/j.bmcl.2017.06.009 Staphylococcus aureus 4
28610977 10.1016/j.bmcl.2017.06.009 Unchecked 2
28610977 10.1016/j.bmcl.2017.06.009 No relevant target 1

Data from ChEMBL 36 via Core Engine