Assay Detail
Binding
CHEMBL3887316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Methods for assessing the selectively of ACAT1 inhibitors are known in the art and can be based upon any conventional assay including, but not limited to the determination of the half maximal (50%) inhibitory concentration (IC) of a substance (i.e., 50% IC, or IC50), the binding affinity of the inhibitor (i.e., Ki), and/or the half maximal effective concentration (EC50) of the inhibitor for ACAT1 as compared to ACAT2. See, e.g., Lada, et al. (2004) J. Lipid Res. 45:378-386 and U.S. Pat. No. 5,968,749. ACAT1 and ACAT2 proteins that can be employed in such assays are well-known in the art and set forth, e.g., in GENBANK Accession Nos. NP-000010 (human ACAT1) and NP-005882 (human ACAT2). See also U.S. Pat. No. 5,834,283.
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Method for selectively inhibiting ACAT1 in the treatment of alzheimer's disease
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.44 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1908306 | EFLUCIMIBE | 2.0 | 1 | 6.96 |
| CHEMBL3894947 | — | — | 1 | 6.56 |
| CHEMBL3899908 | — | — | 1 | 6.28 |
| CHEMBL3936899 | — | — | 1 | 6.22 |
| CHEMBL3905226 | — | — | 1 | 5.82 |
| CHEMBL516093 | BEAUVERIOLIDE I | — | 1 | 4.70 |
| CHEMBL3912464 | — | — | 1 | 4.28 |
| CHEMBL3941615 | — | — | 1 | 4.12 |
| CHEMBL3936896 | — | — | 1 | 4.01 |
| CHEMBL3890942 | — | — | 1 | - |
| CHEMBL409855 | BEAUVERIOLIDE III | — | 1 | - |
| CHEMBL408322 | — | — | 1 | - |
| CHEMBL270041 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1908306 | EFLUCIMIBE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3894947 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL3899908 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3936899 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3905226 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL516093 | BEAUVERIOLIDE I | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3912464 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL3941615 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL3936896 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL3890942 | — | IC50 | = | 102850.0 | nM | - |
| CHEMBL409855 | BEAUVERIOLIDE III | IC50 | > | 20000.0 | nM | - |
| CHEMBL408322 | — | IC50 | = | 230000.0 | nM | - |
| CHEMBL270041 | — | IC50 | = | 414000.0 | nM | - |