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Assay Detail

CHEMBL865343

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Binding
Inhibitory activity against Staphylococcus aureus ATCC 29213 wild type Topo 4
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA topoisomerase 4 subunit A (CHEMBL4088)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
Wiles JA, Song Y, Wang Q, Lucien E, Hashimoto A, Cheng J, Marlor CW, Ou Y, Podos SD, Thanassi JA, Thoma CL, Deshpande M, Pucci MJ, Bradbury BJ.
Bioorg Med Chem Lett (2006) 16 : 1277 -1281
PubMed 16337789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.12 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203557 1 6.30
CHEMBL205110 1 6.16
CHEMBL32 MOXIFLOXACIN 4.0 1 6.10
CHEMBL8 CIPROFLOXACIN 4.0 1 6.00
CHEMBL203491 1 5.96
CHEMBL382028 1 5.66
CHEMBL204904 1 5.62
CHEMBL380649 1 5.50
CHEMBL425234 1 5.48
CHEMBL203979 1 5.48
CHEMBL204762 1 5.48
CHEMBL379022 1 5.46
CHEMBL204544 1 5.44
CHEMBL202753 1 5.44
CHEMBL204911 1 5.32
CHEMBL380533 1 5.30
CHEMBL381257 1 5.20
CHEMBL204749 1 5.10
CHEMBL206622 1 5.07
CHEMBL203851 1 5.00
CHEMBL203935 1 5.00
CHEMBL204230 1 4.92
CHEMBL378608 1 4.85
CHEMBL206553 1 4.80
CHEMBL381833 1 4.80
CHEMBL204899 1 4.75
CHEMBL382247 1 4.72
CHEMBL206156 1 4.68
CHEMBL382172 1 4.64
CHEMBL202813 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203557 IC50 = 500.0 nM 6.30
CHEMBL205110 IC50 = 700.0 nM 6.16
CHEMBL32 MOXIFLOXACIN IC50 = 800.0 nM 6.10
CHEMBL8 CIPROFLOXACIN IC50 = 1000.0 nM 6.00
CHEMBL203491 IC50 = 1100.0 nM 5.96
CHEMBL382028 IC50 = 2200.0 nM 5.66
CHEMBL204904 IC50 = 2400.0 nM 5.62
CHEMBL380649 IC50 = 3200.0 nM 5.50
CHEMBL425234 IC50 = 3300.0 nM 5.48
CHEMBL203979 IC50 = 3300.0 nM 5.48
CHEMBL204762 IC50 = 3300.0 nM 5.48
CHEMBL379022 IC50 = 3500.0 nM 5.46
CHEMBL204544 IC50 = 3600.0 nM 5.44
CHEMBL202753 IC50 = 3600.0 nM 5.44
CHEMBL204911 IC50 = 4800.0 nM 5.32
CHEMBL380533 IC50 = 5000.0 nM 5.30
CHEMBL381257 IC50 = 6300.0 nM 5.20
CHEMBL204749 IC50 = 8000.0 nM 5.10
CHEMBL206622 IC50 = 8500.0 nM 5.07
CHEMBL203935 IC50 = 10000.0 nM 5.00
CHEMBL203851 IC50 = 9900.0 nM 5.00
CHEMBL204230 IC50 = 12000.0 nM 4.92
CHEMBL378608 IC50 = 14000.0 nM 4.85
CHEMBL206553 IC50 = 16000.0 nM 4.80
CHEMBL381833 IC50 = 16000.0 nM 4.80
CHEMBL204899 IC50 = 18000.0 nM 4.75
CHEMBL382247 IC50 = 19000.0 nM 4.72
CHEMBL206156 IC50 = 21000.0 nM 4.68
CHEMBL382172 IC50 = 23000.0 nM 4.64
CHEMBL437129 IC50 = 26000.0 nM 4.58
CHEMBL202813 IC50 = 26000.0 nM 4.58
CHEMBL378604 IC50 = 29000.0 nM 4.54
CHEMBL425233 IC50 = 33000.0 nM 4.48
CHEMBL442792 IC50 = 42000.0 nM 4.38
CHEMBL383328 IC50 = 48000.0 nM 4.32
CHEMBL204346 IC50 = 50000.0 nM 4.30
CHEMBL202633 IC50 = 64000.0 nM 4.19
CHEMBL383001 IC50 > 40000.0 nM -
CHEMBL204042 IC50 > 38000.0 nM -
CHEMBL204320 IC50 > 40000.0 nM -