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Compound Detail

CHEMBL2011390

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COc1cc(Br)cc(/C=C2\SC(=S)N(CCC(=O)O)C2=O)c1O

Basic Information

ChEMBL ID CHEMBL2011390
Phase Preclinical
Structure Type MOL
InChI Key WLOBMDQLCHTQOX-YHYXMXQVSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

418.3
MW (Da)
2.84
ALogP
6
HBA
2
HBD
87.1
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H12BrNO5S2
MW 418.29
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -1.26

Activity Summary

IC50 1 meas. best 4.16
Kd 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.16 4.16 70000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 70000.0 nM 4.16 Inhibition of Escherichia coli DNA gyrase B using relaxed pNO1 as substrate afte... 22444877

Literature References

PubMed DOI Target Context # Activities
22444877 10.1016/j.bmc.2012.02.052 Unchecked 2
22444877 10.1016/j.bmc.2012.02.052 Staphylococcus aureus 1
22444877 10.1016/j.bmc.2012.02.052 Enterococcus faecalis 1
22444877 10.1016/j.bmc.2012.02.052 Haemophilus influenzae 1

Data from ChEMBL 36 via Core Engine