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Compound Detail

CHEMBL3742285

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CCCc1cccc2c(-c3cnc(-c4ccc(C(=O)O)c(F)c4)s3)n[nH]c12

Basic Information

ChEMBL ID CHEMBL3742285
Phase Preclinical
Structure Type MOL
InChI Key PXRYYFCIQFITSS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

381.4
MW (Da)
5.14
ALogP
4
HBA
2
HBD
78.9
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16FN3O2S
MW 381.43
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 42.0 mL.min-1.kg-1 Mus musculus
T1/2 2.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1300.0 nM 5.89 Inhibition of Staphylococcus aureus topoisomerase 4 by fluorescence analysis 26487916

Literature References

PubMed DOI Target Context # Activities
26487916 10.1021/acsmedchemlett.5b00266 Staphylococcus aureus 4
26487916 10.1021/acsmedchemlett.5b00266 Mus musculus 4
26487916 10.1021/acsmedchemlett.5b00266 Streptococcus pneumoniae 3
26487916 10.1021/acsmedchemlett.5b00266 DNA gyrase subunit B 1
26487916 10.1021/acsmedchemlett.5b00266 Unchecked 1
26487916 10.1021/acsmedchemlett.5b00266 Enterococcus faecium 1
26487916 10.1021/acsmedchemlett.5b00266 Enterococcus faecalis 1

Data from ChEMBL 36 via Core Engine