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Assay Detail

CHEMBL5146134

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

Toxicity
Inhibition of human ERG by Ionworks electrophysiology assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 20 5.09 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205047 1 5.52
CHEMBL5182200 1 5.40
CHEMBL5201228 1 5.30
CHEMBL5184352 1 5.30
CHEMBL5194618 1 5.16
CHEMBL5199405 1 5.16
CHEMBL5172094 1 5.05
CHEMBL5190832 1 5.00
CHEMBL5195721 1 4.89
CHEMBL5206169 1 4.70
CHEMBL5184104 1 4.50
CHEMBL5177076 1 -
CHEMBL5198597 1 -
CHEMBL5188163 1 -
CHEMBL5170129 1 -
CHEMBL5172158 1 -
CHEMBL5195268 1 -
CHEMBL5195428 1 -
CHEMBL3317856 GEPOTIDACIN 3.0 1 -
CHEMBL8 CIPROFLOXACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205047 IC50 = 3000.0 nM 5.52
CHEMBL5182200 IC50 = 4000.0 nM 5.40
CHEMBL5201228 IC50 = 5000.0 nM 5.30
CHEMBL5184352 IC50 = 5000.0 nM 5.30
CHEMBL5194618 IC50 = 7000.0 nM 5.16
CHEMBL5199405 IC50 = 7000.0 nM 5.16
CHEMBL5172094 IC50 = 9000.0 nM 5.05
CHEMBL5190832 IC50 = 10000.0 nM 5.00
CHEMBL5195721 IC50 = 13000.0 nM 4.89
CHEMBL5206169 IC50 = 20000.0 nM 4.70
CHEMBL5184104 IC50 = 32000.0 nM 4.50
CHEMBL5177076 IC50 > 100000.0 nM -
CHEMBL5198597 IC50 > 100000.0 nM -
CHEMBL5188163 IC50 - -
CHEMBL5170129 IC50 > 32000.0 nM -
CHEMBL5172158 IC50 > 100000.0 nM -
CHEMBL5195268 IC50 > 100000.0 nM -
CHEMBL5195428 IC50 - -
CHEMBL3317856 GEPOTIDACIN IC50 > 100000.0 nM -
CHEMBL8 CIPROFLOXACIN IC50 > 100000.0 nM -