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Compound Detail

CHEMBL4870243

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Cc1[nH]c(C(=O)Nc2nc3c(OCc4ccccc4)cc(C(=O)NCC#N)cc3s2)c(Cl)c1Cl

Basic Information

ChEMBL ID CHEMBL4870243
Phase Preclinical
Structure Type MOL
InChI Key KTDQGQFRRTZMBJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

514.4
MW (Da)
5.32
ALogP
6
HBA
3
HBD
119.9
PSA (Ų)
0.29
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H17Cl2N5O3S
MW 514.39
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.81

Activity Summary

IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL3038482
IC50 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 180.0 nM 6.75 Inhibition of Staphylococcus aureus DNA gyrase assessed reduction in relaxation ... 33524686

Literature References

PubMed DOI Target Context # Activities
33524686 10.1016/j.ejmech.2021.113200 DNA gyrase 2
33524686 10.1016/j.ejmech.2021.113200 Unchecked 2
33524686 10.1016/j.ejmech.2021.113200 Staphylococcus aureus 2
33524686 10.1016/j.ejmech.2021.113200 Enterococcus faecalis 1
33524686 10.1016/j.ejmech.2021.113200 Acinetobacter baumannii 1
33524686 10.1016/j.ejmech.2021.113200 Pseudomonas aeruginosa 1
33524686 10.1016/j.ejmech.2021.113200 Klebsiella pneumoniae 1
33524686 10.1016/j.ejmech.2021.113200 Escherichia coli 1

Data from ChEMBL 36 via Core Engine