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Assay Detail

CHEMBL878432

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Binding
In vitro inhibitory activity against Holo-[acyl-carrier-protein] synthase was determined using Bacillus subtilis GST-Acp-HTRFassay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus subtilis
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Holo-[acyl-carrier-protein] synthase (CHEMBL4734)
Type SINGLE PROTEIN
Organism Bacillus subtilis (strain 168)

Publication

Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.
Gilbert AM, Kirisits M, Toy P, Nunn DS, Failli A, Dushin EG, Novikova E, Petersen PJ, Joseph-McCarthy D, McFadyen I, Fritz CC.
Bioorg Med Chem Lett (2004) 14 : 37 -41
PubMed 14684293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.70 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130657 1 6.89
CHEMBL335756 1 6.57
CHEMBL130683 1 6.08
CHEMBL130278 1 5.96
CHEMBL130832 1 5.89
CHEMBL129980 1 5.82
CHEMBL130279 1 5.72
CHEMBL435599 1 5.70
CHEMBL339848 1 5.68
CHEMBL339849 1 5.47
CHEMBL132893 1 4.82
CHEMBL133301 1 4.82
CHEMBL133577 1 4.70
CHEMBL133468 1 -
CHEMBL131492 1 -
CHEMBL134062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130657 IC50 = 130.0 nM 6.89
CHEMBL335756 IC50 = 270.0 nM 6.57
CHEMBL130683 IC50 = 830.0 nM 6.08
CHEMBL130278 IC50 = 1100.0 nM 5.96
CHEMBL130832 IC50 = 1300.0 nM 5.89
CHEMBL129980 IC50 = 1500.0 nM 5.82
CHEMBL130279 IC50 = 1900.0 nM 5.72
CHEMBL435599 IC50 = 2000.0 nM 5.70
CHEMBL339848 IC50 = 2100.0 nM 5.68
CHEMBL339849 IC50 = 3400.0 nM 5.47
CHEMBL132893 IC50 = 15000.0 nM 4.82
CHEMBL133301 IC50 = 15000.0 nM 4.82
CHEMBL133577 IC50 = 20000.0 nM 4.70
CHEMBL133468 IC50 > 20000.0 nM -
CHEMBL131492 IC50 > 20000.0 nM -
CHEMBL134062 IC50 > 20000.0 nM -