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Assay Detail

CHEMBL5223485

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

Functional
Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing the green fluorescence protein infected in mouse RAW264.7 cells assessed as inhibition of bacterial growth pre-infected with cell followed by compound addition and measured after 5 days by Hoechst 33342 staining based analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mycobacterium tuberculosis
Cell Type RAW264.7
Confidence 1 — Organism
Curated By Autocuration

Target

Mycobacterium tuberculosis (CHEMBL360)
Type ORGANISM
Organism Mycobacterium tuberculosis

Publication

Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent.
Jin G, Mi Kim Y, Lee A, Choi J, Kang S, Seo M, Jea Seo J, Lee S, Kang J, Kim J, Park S, Woo M, Falcão VCA, Lee H, Heo J, Shum D, Park K, Delorme V, Choi I.
Bioorg Med Chem (2020) 28 : 115797 -115797
PubMed 33075682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.52 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374478 RIFAMPIN 4.0 1 7.22
CHEMBL5271330 1 7.00
CHEMBL5289264 1 6.96
CHEMBL5282383 1 6.96
CHEMBL5283928 1 6.77
CHEMBL5268713 1 6.72
CHEMBL5267910 1 6.72
CHEMBL5280742 1 6.70
CHEMBL5272617 1 6.68
CHEMBL5283107 1 6.68
CHEMBL5289282 1 6.68
CHEMBL5279170 1 6.64
CHEMBL5276526 1 6.60
CHEMBL5284665 1 6.57
CHEMBL5274019 1 6.51
CHEMBL5273568 1 6.48
CHEMBL64 ISONIAZID 4.0 1 6.46
CHEMBL5290102 1 6.44
CHEMBL5270444 1 6.43
CHEMBL5288259 1 6.34
CHEMBL5281280 1 6.33
CHEMBL5273175 1 6.29
CHEMBL5283080 1 6.16
CHEMBL5268032 1 5.89
CHEMBL5267127 1 5.68
CHEMBL5290680 1 5.56
CHEMBL5288054 1 -
CHEMBL5272865 1 -
CHEMBL5284586 1 -
CHEMBL5281858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374478 RIFAMPIN IC50 = 60.0 nM 7.22
CHEMBL5271330 IC50 = 100.0 nM 7.00
CHEMBL5289264 IC50 = 110.0 nM 6.96
CHEMBL5282383 IC50 = 110.0 nM 6.96
CHEMBL5283928 IC50 = 170.0 nM 6.77
CHEMBL5268713 IC50 = 190.0 nM 6.72
CHEMBL5267910 IC50 = 190.0 nM 6.72
CHEMBL5280742 IC50 = 200.0 nM 6.70
CHEMBL5272617 IC50 = 210.0 nM 6.68
CHEMBL5283107 IC50 = 210.0 nM 6.68
CHEMBL5289282 IC50 = 210.0 nM 6.68
CHEMBL5279170 IC50 = 230.0 nM 6.64
CHEMBL5276526 IC50 = 250.0 nM 6.60
CHEMBL5284665 IC50 = 270.0 nM 6.57
CHEMBL5274019 IC50 = 310.0 nM 6.51
CHEMBL5273568 IC50 = 330.0 nM 6.48
CHEMBL64 ISONIAZID IC50 = 350.0 nM 6.46
CHEMBL5290102 IC50 = 360.0 nM 6.44
CHEMBL5270444 IC50 = 370.0 nM 6.43
CHEMBL5288259 IC50 = 460.0 nM 6.34
CHEMBL5281280 IC50 = 470.0 nM 6.33
CHEMBL5273175 IC50 = 510.0 nM 6.29
CHEMBL5283080 IC50 = 700.0 nM 6.16
CHEMBL5268032 IC50 = 1300.0 nM 5.89
CHEMBL5267127 IC50 = 2100.0 nM 5.68
CHEMBL5290680 IC50 = 2750.0 nM 5.56
CHEMBL5288054 IC50 > 20000.0 nM -
CHEMBL5272865 IC50 > 20000.0 nM -
CHEMBL5284586 IC50 > 20000.0 nM -
CHEMBL5281858 IC50 > 20000.0 nM -
CHEMBL5276367 IC50 > 20000.0 nM -