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Assay Detail

CHEMBL2049313

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

Binding
Inhibition of Mycobacterium tuberculosis RNA polymerase D435V mutant by rolling circle transcription assay in the presence of sigmaA factor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
Gill SK, Xu H, Kirchhoff PD, Cierpicki T, Turbiak AJ, Wan B, Zhang N, Peng KW, Franzblau SG, Garcia GA, Showalter HD.
J Med Chem (2012) 55 : 3814 -3826
PubMed 22452568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.88 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2046886 1 5.05
CHEMBL2046887 1 4.89
CHEMBL2046885 1 4.70
CHEMBL236297 RIFALAZIL 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2046886 IC50 = 9000.0 nM 5.05
CHEMBL2046887 IC50 = 13000.0 nM 4.89
CHEMBL2046885 IC50 = 20000.0 nM 4.70
CHEMBL236297 RIFALAZIL IC50 = 541000.0 nM -