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Assay Detail

CHEMBL940953

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Binding
Inhibition of Mycobacterium tuberculosis FabH
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mycobacterial beta-ketoacyl-[acyl-carrier-protein] synthase III (CHEMBL3640)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Synthesis and biological evaluation of a C5-biphenyl thiolactomycin library.
Bhowruth V, Brown AK, Senior SJ, Snaith JS, Besra GS.
Bioorg Med Chem Lett (2007) 17 : 5643 -5646
PubMed 17766110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.69 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250431 1 5.52
CHEMBL399477 1 5.40
CHEMBL250429 1 5.16
CHEMBL250630 1 4.82
CHEMBL249805 1 4.27
CHEMBL250819 1 4.17
CHEMBL399043 THIOLACTOMYCIN 1 4.12
CHEMBL250824 1 4.07
CHEMBL251035 1 -
CHEMBL400501 1 -
CHEMBL250823 1 -
CHEMBL250818 1 -
CHEMBL401380 1 -
CHEMBL249417 1 -
CHEMBL249210 1 -
CHEMBL400279 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250431 IC50 = 3000.0 nM 5.52
CHEMBL399477 IC50 = 4000.0 nM 5.40
CHEMBL250429 IC50 = 7000.0 nM 5.16
CHEMBL250630 IC50 = 15000.0 nM 4.82
CHEMBL249805 IC50 = 54000.0 nM 4.27
CHEMBL250819 IC50 = 68000.0 nM 4.17
CHEMBL399043 THIOLACTOMYCIN IC50 = 75000.0 nM 4.12
CHEMBL250824 IC50 = 86000.0 nM 4.07
CHEMBL251035 IC50 = 130000.0 nM -
CHEMBL400501 IC50 = 283000.0 nM -
CHEMBL250823 IC50 = 200000.0 nM -
CHEMBL250818 IC50 = 105000.0 nM -
CHEMBL401380 IC50 = 207000.0 nM -
CHEMBL249417 IC50 = 135000.0 nM -
CHEMBL249210 IC50 = 150000.0 nM -
CHEMBL400279 IC50 = 156000.0 nM -