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Assay Detail

CHEMBL648365

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

Binding
Inhibitory activity against recombinant Mycobacterium tuberculosis beta-ketoacyl-Acyl Carrier Protein synthase mtFabH condensing enzyme
9
Total Activities
9
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

Acetylene-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 (2004) 14 : 373 -376
PubMed 14698162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.62 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339331 1 5.40
CHEMBL124012 1 5.16
CHEMBL333744 1 5.16
CHEMBL124220 1 4.77
CHEMBL126054 1 4.47
CHEMBL124086 1 4.32
CHEMBL399043 THIOLACTOMYCIN 1 4.13
CHEMBL123723 1 4.13
CHEMBL122046 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339331 IC50 = 4000.0 nM 5.40
CHEMBL124012 IC50 = 7000.0 nM 5.16
CHEMBL333744 IC50 = 7000.0 nM 5.16
CHEMBL124220 IC50 = 17000.0 nM 4.77
CHEMBL126054 IC50 = 34000.0 nM 4.47
CHEMBL124086 IC50 = 48000.0 nM 4.32
CHEMBL399043 THIOLACTOMYCIN IC50 = 74900.0 nM 4.13
CHEMBL123723 IC50 = 74000.0 nM 4.13
CHEMBL122046 IC50 = 100000.0 nM 4.00