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Compound Detail

CHEMBL4126781

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COc1c(Cl)c(OC)c2c(c1C(C)=O)OC(C)(C)C(OC)C2Cl

Basic Information

ChEMBL ID CHEMBL4126781
Phase Preclinical
Structure Type MOL
InChI Key QTISQBZFCNUZBT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

363.2
MW (Da)
4.03
ALogP
5
HBA
0
HBD
54.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H20Cl2O5
MW 363.24
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness 1.54

Activity Summary

IC50 1 meas. best 8.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL3038482
IC50 8.73 8.73 1.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 1.86 nM 8.73 Inhibition of Staphylococcus aureus DNA gyrase assessed as reduction in relaxati... 29803359

Literature References

PubMed DOI Target Context # Activities
29803359 10.1016/j.bmc.2018.05.016 Erythrocyte 3
29803359 10.1016/j.bmc.2018.05.016 DNA gyrase 2
29803359 10.1016/j.bmc.2018.05.016 Corynebacterium diphtheriae 2
29803359 10.1016/j.bmc.2018.05.016 Klebsiella pneumoniae 1
29803359 10.1016/j.bmc.2018.05.016 Escherichia coli 1
29803359 10.1016/j.bmc.2018.05.016 Pseudomonas aeruginosa 1
29803359 10.1016/j.bmc.2018.05.016 Staphylococcus aureus 1
29803359 10.1016/j.bmc.2018.05.016 Streptococcus pyogenes 1

Data from ChEMBL 36 via Core Engine