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Assay Detail

CHEMBL5146148

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Binding
Inhibition of human topoisomerase 2 assessed as reduction in decatenation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA topoisomerase 2-alpha (CHEMBL1806)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.
Lyons A, Kirkham J, Blades K, Orr D, Dauncey E, Smith O, Dick E, Walker R, Matthews T, Bunt A, Finlayson J, Morrison I, Savage VJ, Moyo E, Butler HS, Newman R, Ooi N, Smith A, Charrier C, Ratcliffe AJ, Stokes NR, Best S, Salisbury AM, Craighead M, Cooper IR.
Bioorg Med Chem Lett (2022) 65 : 128648 -128648
PubMed 35231579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.41 4.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201228 1 4.84
CHEMBL3317856 GEPOTIDACIN 3.0 1 4.26
CHEMBL5195268 1 4.14
CHEMBL8 CIPROFLOXACIN 4.0 1 -
CHEMBL5184104 1 -
CHEMBL5172158 1 -
CHEMBL5182200 1 -
CHEMBL5198597 1 -
CHEMBL5177076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201228 IC50 = 14400.0 nM 4.84
CHEMBL3317856 GEPOTIDACIN IC50 = 55200.0 nM 4.26
CHEMBL5195268 IC50 = 72800.0 nM 4.14
CHEMBL8 CIPROFLOXACIN IC50 > 100000.0 nM -
CHEMBL5184104 IC50 > 100000.0 nM -
CHEMBL5172158 IC50 > 100000.0 nM -
CHEMBL5182200 IC50 > 100000.0 nM -
CHEMBL5198597 IC50 > 100000.0 nM -
CHEMBL5177076 IC50 > 100000.0 nM -