Assay Detail
Binding
CHEMBL3101031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Escherichia coli FabH overexpressed in Escherichia coli DH10B cells assessed as incorporation of [3H] in the product after 25 mins by liquid scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-oxoacyl-[acyl-carrier-protein] synthase 3 (CHEMBL1795135) ↗| Type | SINGLE PROTEIN |
| Organism | Escherichia coli |
Publication
Design, synthesis and antibacterial activities of 5-(pyrazin-2-yl)-4H-1,2,4-triazole-3-thiol derivatives containing Schiff base formation as FabH inhibitory.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.72 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3098259 | — | — | 1 | 5.28 |
| CHEMBL176 | BEKANAMYCIN | 3.0 | 1 | 5.20 |
| CHEMBL3098253 | — | — | 1 | 4.89 |
| CHEMBL3098254 | — | — | 1 | 4.82 |
| CHEMBL3098255 | — | — | 1 | 4.64 |
| CHEMBL3098261 | — | — | 1 | 4.61 |
| CHEMBL3098267 | — | — | 1 | 4.57 |
| CHEMBL3098258 | — | — | 1 | 4.53 |
| CHEMBL3098252 | — | — | 1 | 4.34 |
| CHEMBL3098260 | — | — | 1 | 4.32 |
| CHEMBL3098271 | — | — | 1 | - |
| CHEMBL3098266 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3098259 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL176 | BEKANAMYCIN | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3098253 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL3098254 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL3098255 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL3098261 | — | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL3098267 | — | IC50 | = | 27100.0 | nM | 4.57 |
| CHEMBL3098258 | — | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL3098252 | — | IC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL3098260 | — | IC50 | = | 48300.0 | nM | 4.32 |
| CHEMBL3098271 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3098266 | — | IC50 | > | 100000.0 | nM | - |