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Assay Detail

CHEMBL3745476

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Binding
Inhibition of Staphylococcus aureus Gyrase B ATPase activity by fluorescence analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA gyrase subunit B (CHEMBL1921666)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA, Ryan D, Lippa B, Dolle RE.
ACS Med Chem Lett (2015) 6 : 1080 -1085
PubMed 26487916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.63 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3741798 1 8.10
CHEMBL3739786 1 8.05
CHEMBL3741350 1 8.05
CHEMBL3741270 1 8.00
CHEMBL3739453 1 7.96
CHEMBL3739840 1 7.96
CHEMBL3742199 1 7.96
CHEMBL3741475 1 7.92
CHEMBL3741905 1 7.89
CHEMBL3739628 1 7.89
CHEMBL3741327 1 7.85
CHEMBL3739780 1 7.82
CHEMBL3739580 1 7.82
CHEMBL3739684 1 7.70
CHEMBL3741416 1 7.60
CHEMBL3740656 1 7.54
CHEMBL3742250 1 7.31
CHEMBL3741742 1 7.28
CHEMBL3741635 1 6.78
CHEMBL3739906 1 5.19
CHEMBL3741151 1 -
CHEMBL3742285 1 -
CHEMBL3741177 1 -
CHEMBL3740258 1 -
CHEMBL3741250 1 -
CHEMBL3740365 1 -
CHEMBL3741066 1 -
CHEMBL3742072 1 -
CHEMBL3741453 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3741798 IC50 = 8.0 nM 8.10
CHEMBL3739786 IC50 = 9.0 nM 8.05
CHEMBL3741350 IC50 = 9.0 nM 8.05
CHEMBL3741270 IC50 = 10.0 nM 8.00
CHEMBL3739453 IC50 = 11.0 nM 7.96
CHEMBL3739840 IC50 = 11.0 nM 7.96
CHEMBL3742199 IC50 = 11.0 nM 7.96
CHEMBL3741475 IC50 = 12.0 nM 7.92
CHEMBL3741905 IC50 = 13.0 nM 7.89
CHEMBL3739628 IC50 = 13.0 nM 7.89
CHEMBL3741327 IC50 = 14.0 nM 7.85
CHEMBL3739780 IC50 = 15.0 nM 7.82
CHEMBL3739580 IC50 = 15.0 nM 7.82
CHEMBL3739684 IC50 = 20.0 nM 7.70
CHEMBL3741416 IC50 = 25.0 nM 7.60
CHEMBL3740656 IC50 = 29.0 nM 7.54
CHEMBL3742250 IC50 = 49.0 nM 7.31
CHEMBL3741742 IC50 = 52.0 nM 7.28
CHEMBL3741635 IC50 = 168.0 nM 6.78
CHEMBL3739906 IC50 = 6500.0 nM 5.19
CHEMBL3741151 IC50 < 8.0 nM -
CHEMBL3742285 IC50 < 8.0 nM -
CHEMBL3741177 IC50 < 8.0 nM -
CHEMBL3740258 IC50 < 8.0 nM -
CHEMBL3741250 IC50 < 8.0 nM -
CHEMBL3740365 IC50 < 8.0 nM -
CHEMBL3741066 IC50 < 8.0 nM -
CHEMBL3742072 IC50 < 8.0 nM -
CHEMBL3741453 IC50 < 8.0 nM -