Assay Detail
Binding
CHEMBL5549254
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Catalytic inhibition of Acanthamoeba castellanii CYP51 expressed in Escherichia coli HMS-174 (DE3) cells assessed as inhibition of substrate induced 14alpha-demthylation using obtusifoliol as substrate incubated for 1 hr in presence of NADPH-CYP450 reductase by RP-HPLC analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Acanthamoeba castellanii |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of Potent and Selective Inhibitors of <i>Acanthamoeba</i>: Structural Insights into Sterol 14α-Demethylase as a Key Drug Target.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.57 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3311228 | OTESECONAZOLE | 4.0 | 1 | 6.70 |
| CHEMBL4594426 | VT-1598 | 1.0 | 1 | 6.60 |
| CHEMBL638 | VORICONAZOLE | 4.0 | 1 | 6.35 |
| CHEMBL3104375 | — | — | 1 | 5.89 |
| CHEMBL3104526 | — | — | 1 | 5.26 |
| CHEMBL4128885 | — | — | 1 | 4.69 |
| CHEMBL1236677 | — | — | 1 | 4.56 |
| CHEMBL3629567 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3311228 | OTESECONAZOLE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4594426 | VT-1598 | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL638 | VORICONAZOLE | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3104375 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3104526 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4128885 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL1236677 | — | IC50 | = | 27300.0 | nM | 4.56 |
| CHEMBL3629567 | — | IC50 | = | 28900.0 | nM | 4.54 |