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Assay Detail

CHEMBL3389999

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Staphylococcus aureus topoisomerase 4 assessed as reduction in decatenation of kDNA at 100 to 500 uM by gel electrophoresis method
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Perlmutter JI, Forbes LT, Krysan DJ, Ebsworth-Mojica K, Colquhoun JM, Wang JL, Dunman PM, Flaherty DP.
J Med Chem (2014) 57 : 8540 -8562
PubMed 25238555 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 4.28 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8 CIPROFLOXACIN 4.0 1 5.40
CHEMBL432527 1 4.00
CHEMBL3342831 1 4.00
CHEMBL3342826 1 4.00
CHEMBL3342828 1 4.00
CHEMBL3343207 1 -
CHEMBL3342818 1 -
CHEMBL3343208 1 -
CHEMBL3343209 1 -
CHEMBL3343210 1 -
CHEMBL3343216 1 -
CHEMBL3344284 1 -
CHEMBL3344285 1 -
CHEMBL3344385 1 -
CHEMBL3342827 1 -
CHEMBL3342816 1 -
CHEMBL3342817 1 -
CHEMBL3343206 1 -
CHEMBL3343205 1 -
CHEMBL3343204 1 -
CHEMBL3343203 1 -
CHEMBL3343202 1 -
CHEMBL3343201 1 -
CHEMBL3343200 1 -
CHEMBL3343199 1 -
CHEMBL3343198 1 -
CHEMBL3343196 1 -
CHEMBL3343195 1 -
CHEMBL303454 R-TERFENADINE 1 -
CHEMBL3343194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8 CIPROFLOXACIN IC50 = 4000.0 nM 5.40
CHEMBL432527 IC50 = 100000.0 nM 4.00
CHEMBL3342831 IC50 = 100000.0 nM 4.00
CHEMBL3342826 IC50 = 100000.0 nM 4.00
CHEMBL3342828 IC50 = 100000.0 nM 4.00
CHEMBL3342816 IC50 = 273000.0 nM -
CHEMBL205154 TERFENADONE IC50 = 110000.0 nM -
CHEMBL3342817 IC50 > 333000.0 nM -
CHEMBL3342818 IC50 > 333000.0 nM -
CHEMBL3342819 IC50 > 333000.0 nM -
CHEMBL3342820 IC50 > 333000.0 nM -
CHEMBL3342821 IC50 > 333000.0 nM -
CHEMBL3342822 IC50 > 333000.0 nM -
CHEMBL3342823 IC50 > 333000.0 nM -
CHEMBL3342824 IC50 = 133000.0 nM -
CHEMBL3342825 IC50 = 333000.0 nM -
CHEMBL3343193 IC50 = 133000.0 nM -
CHEMBL3342829 IC50 > 333000.0 nM -
CHEMBL914 FEXOFENADINE IC50 > 333000.0 nM -
CHEMBL3342830 IC50 = 320000.0 nM -
CHEMBL3342832 IC50 = 147000.0 nM -
CHEMBL3342833 IC50 = 213000.0 nM -
CHEMBL3342834 IC50 = 250000.0 nM -
CHEMBL3342835 IC50 > 333000.0 nM -
CHEMBL3342836 IC50 > 333000.0 nM -
CHEMBL17157 TERFENADINE IC50 = 206000.0 nM -
CHEMBL3343204 IC50 > 333000.0 nM -
CHEMBL3343194 IC50 = 247000.0 nM -
CHEMBL303454 R-TERFENADINE IC50 = 110000.0 nM -
CHEMBL3343195 IC50 > 333000.0 nM -
CHEMBL3343196 IC50 > 333000.0 nM -
CHEMBL3343198 IC50 > 333000.0 nM -
CHEMBL3343199 IC50 = 267000.0 nM -
CHEMBL3343200 IC50 = 260000.0 nM -
CHEMBL3343201 IC50 > 333000.0 nM -
CHEMBL3343202 IC50 > 333000.0 nM -
CHEMBL3343203 IC50 > 333000.0 nM -
CHEMBL3342827 IC50 > 333000.0 nM -
CHEMBL3343205 IC50 > 333000.0 nM -
CHEMBL3343206 IC50 > 333000.0 nM -
CHEMBL3343207 IC50 = 133000.0 nM -
CHEMBL3343208 IC50 = 227000.0 nM -
CHEMBL3343209 IC50 = 280000.0 nM -
CHEMBL3343210 IC50 > 333000.0 nM -
CHEMBL3343216 IC50 = 160000.0 nM -
CHEMBL3344284 IC50 > 333000.0 nM -
CHEMBL3344285 IC50 > 333000.0 nM -
CHEMBL3344385 IC50 = 160000.0 nM -