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Compound Detail

CHEMBL2158047

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COc1ccc2nccc([C@@H](O)CC[C@@H]3CCN(CCSc4ccc(C#N)[se]4)C[C@@H]3C(=O)O)c2c1

Basic Information

ChEMBL ID CHEMBL2158047
Phase Preclinical
Structure Type MOL
InChI Key HIVIYQQTTLILJI-UWSIMGETSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

558.6
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N3O4SSe
MW 558.56

Activity Summary

IC50 1 meas. best 4.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA gyrase
CHEMBL3038482
IC50 4.44 4.44 36600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA gyrase IC50 = 36600.0 nM 4.44 Inhibition of Staphylococcus aureus DNA gyrase by supercoiling assay 21443219

Literature References

PubMed DOI Target Context # Activities
21443219 10.1021/jm2002124 Staphylococcus aureus 2
21443219 10.1021/jm2002124 HEp-2 1
21443219 10.1021/jm2002124 Unchecked 1
21443219 10.1021/jm2002124 DNA gyrase 1

Data from ChEMBL 36 via Core Engine