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Assay Detail

CHEMBL2446342

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Binding
Inhibition of Escherichia coli RNA polymerase core enzyme by transcription assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
Hinsberger S, Hüsecken K, Groh M, Negri M, Haupenthal J, Hartmann RW.
J Med Chem (2013) 56 : 8332 -8338
PubMed 24112046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.83 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374478 RIFAMPIN 4.0 1 7.80
CHEMBL2440261 1 4.92
CHEMBL2440259 1 4.57
CHEMBL175848 1 4.44
CHEMBL2440280 1 4.41
CHEMBL242621 1 4.24
CHEMBL2440270 1 4.17
CHEMBL373673 1 4.09
CHEMBL2440275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374478 RIFAMPIN IC50 = 16.0 nM 7.80
CHEMBL2440261 IC50 = 12000.0 nM 4.92
CHEMBL2440259 IC50 = 27000.0 nM 4.57
CHEMBL175848 IC50 = 36000.0 nM 4.44
CHEMBL2440280 IC50 = 39000.0 nM 4.41
CHEMBL242621 IC50 = 57000.0 nM 4.24
CHEMBL2440270 IC50 = 67000.0 nM 4.17
CHEMBL373673 IC50 = 81000.0 nM 4.09
CHEMBL2440275 IC50 - -