Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL648364

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

Binding
In vitro inhibitory activity against the recombinant Mycobacterium tuberculosis Beta-ketoacyl-ACP synthase III mtFabH condensing enzyme.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenyl-based analogues of thiolactomycin, active against Mycobacterium tuberculosis mtFabH fatty acid condensing enzyme.
Senior SJ, Illarionov PA, Gurcha SS, Campbell IB, Schaeffer ML, Minnikin DE, Besra GS.
Bioorg Med Chem Lett (2003) 13 : 3685 -3688
PubMed 14552758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.44 4.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124220 1 4.77
CHEMBL122848 1 4.72
CHEMBL123594 1 4.60
CHEMBL123181 1 4.54
CHEMBL333571 1 4.37
CHEMBL333742 1 4.29
CHEMBL332364 1 4.28
CHEMBL123595 1 4.28
CHEMBL331347 1 4.13
CHEMBL122699 1 -
CHEMBL123998 1 -
CHEMBL123876 1 -
CHEMBL331729 1 -
CHEMBL333467 1 -
CHEMBL124117 1 -
CHEMBL432983 1 -
CHEMBL332417 1 -
CHEMBL123184 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124220 IC50 = 17000.0 nM 4.77
CHEMBL122848 IC50 = 19000.0 nM 4.72
CHEMBL123594 IC50 = 25000.0 nM 4.60
CHEMBL123181 IC50 = 29000.0 nM 4.54
CHEMBL333571 IC50 = 43000.0 nM 4.37
CHEMBL333742 IC50 = 51000.0 nM 4.29
CHEMBL332364 IC50 = 52000.0 nM 4.28
CHEMBL123595 IC50 = 52000.0 nM 4.28
CHEMBL331347 IC50 = 74900.0 nM 4.13
CHEMBL122699 IC50 = 263000.0 nM -
CHEMBL123998 IC50 = 153000.0 nM -
CHEMBL123876 IC50 > 250000.0 nM -
CHEMBL331729 IC50 = 246000.0 nM -
CHEMBL333467 IC50 = 155000.0 nM -
CHEMBL124117 IC50 = 119000.0 nM -
CHEMBL432983 IC50 = 112000.0 nM -
CHEMBL332417 IC50 = 215000.0 nM -
CHEMBL123184 IC50 > 500000.0 nM -