Assay Detail
Binding
CHEMBL646706
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In vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase in rat hepatic microsomes was measured by using AIV assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: heterocyclic bioisosteres for the urea group in DuP 128
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.70 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274185 | LECIMIBIDE | 2.0 | 1 | 8.00 |
| CHEMBL50132 | — | — | 1 | 7.52 |
| CHEMBL33780 | — | — | 1 | 7.52 |
| CHEMBL298742 | — | — | 1 | 7.40 |
| CHEMBL300506 | — | — | 1 | 7.40 |
| CHEMBL53397 | — | — | 1 | 7.10 |
| CHEMBL54217 | — | — | 1 | 7.10 |
| CHEMBL50131 | — | — | 1 | 7.05 |
| CHEMBL53942 | — | — | 1 | 7.05 |
| CHEMBL54032 | — | — | 1 | 6.85 |
| CHEMBL49993 | — | — | 1 | 6.66 |
| CHEMBL301542 | — | — | 1 | 6.64 |
| CHEMBL53728 | — | — | 1 | 6.52 |
| CHEMBL51087 | — | — | 1 | 6.40 |
| CHEMBL53613 | — | — | 1 | 6.20 |
| CHEMBL51000 | — | — | 1 | 6.16 |
| CHEMBL52911 | — | — | 1 | 6.16 |
| CHEMBL50528 | — | — | 1 | 6.12 |
| CHEMBL51827 | — | — | 1 | 5.85 |
| CHEMBL50359 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274185 | LECIMIBIDE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL50132 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL33780 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL298742 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL300506 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL53397 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL54217 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL50131 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL53942 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL54032 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL49993 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL301542 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL53728 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL51087 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL53613 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL51000 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL52911 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL50528 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL51827 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL50359 | — | IC50 | = | 50000.0 | nM | 4.30 |