Assay Detail
Binding
CHEMBL2401006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged Francisella tularensis SCHU S4 FabI expressed in Escherichia coli BL21 (DE3) using CrCoA as substrate assessed as oxidation of NADH to NAD+ by fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Francisella tularensis subsp. tularensis SCHU S4 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Enoyl-[acyl-carrier-protein] reductase [NADH] (CHEMBL2150835) ↗| Type | SINGLE PROTEIN |
| Organism | Francisella tularensis subsp. tularensis (strain SCHU S4 / Schu 4) |
Publication
3-substituted indole inhibitors against Francisella tularensis FabI identified by structure-based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.53 | 5.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2398664 | — | — | 1 | 5.22 |
| CHEMBL2398663 | — | — | 1 | 4.96 |
| CHEMBL1390649 | — | — | 1 | 4.92 |
| CHEMBL2398662 | — | — | 1 | 4.35 |
| CHEMBL1466 | DICUMAROL | 4.0 | 1 | 4.33 |
| CHEMBL803 | CYTARABINE | 4.0 | 1 | 4.23 |
| CHEMBL990 | BUTENAFINE | 4.0 | 1 | 4.12 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2398664 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2398663 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1390649 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2398662 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL1466 | DICUMAROL | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL803 | CYTARABINE | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL990 | BUTENAFINE | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 79000.0 | nM | 4.10 |