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Assay Detail

CHEMBL2383458

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Binding
Inhibition of rifamycin-resistant Escherichia coli RNA polymerase D516V mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC45
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

DNA-directed RNA polymerase subunit beta (CHEMBL4296294)
Type SINGLE PROTEIN
Organism Escherichia coli O127:H6 (strain E2348/69 / EPEC)

Publication

X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
Molodtsov V, Nawarathne IN, Scharf NT, Kirchhoff PD, Showalter HD, Garcia GA, Murakami KS.
J Med Chem (2013) 56 : 4758 -4763
PubMed 23679862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.85 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2046886 1 5.70
CHEMBL2046885 1 4.46
CHEMBL2046887 1 4.39
CHEMBL236297 RIFALAZIL 3.0 1 -
CHEMBL374478 RIFAMPIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2046886 IC50 = 2000.0 nM 5.70
CHEMBL2046885 IC50 = 35000.0 nM 4.46
CHEMBL2046887 IC50 = 41000.0 nM 4.39
CHEMBL236297 RIFALAZIL IC50 = 204000.0 nM -
CHEMBL374478 RIFAMPIN IC50 = 233000.0 nM -