Assay Detail
Binding
CHEMBL643993
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Inhibitory concentration was evaluated as concentration required to inhibit 50% of the Acyl coenzyme A:cholesterol acyltransferase 1 activity obtained from human THP-1 macrophage enzyme.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Acyl-CoA:Cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.10 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284596 | — | — | 1 | 8.00 |
| CHEMBL284378 | — | — | 1 | 7.30 |
| CHEMBL34219 | — | — | 1 | 7.30 |
| CHEMBL33054 | — | — | 1 | 7.22 |
| CHEMBL286611 | — | — | 1 | 7.16 |
| CHEMBL286434 | — | — | 1 | 7.12 |
| CHEMBL33127 | — | — | 1 | 6.98 |
| CHEMBL286583 | — | — | 1 | 6.89 |
| CHEMBL287233 | — | — | 1 | 6.52 |
| CHEMBL33661 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284596 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL284378 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL34219 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL33054 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL286611 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL286434 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL33127 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL286583 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL287233 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL33661 | — | IC50 | = | 300.0 | nM | 6.52 |