Assay Detail
Binding
CHEMBL642358
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Inhibition of Acyl coenzyme A:cholesterol acyltransferase in J774 Macrophage cell culture
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | Macrophage |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 33 | 6.29 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53728 | — | — | 1 | 7.70 |
| CHEMBL52006 | — | — | 1 | 7.30 |
| CHEMBL50131 | — | — | 1 | 7.22 |
| CHEMBL53397 | — | — | 1 | 7.16 |
| CHEMBL54217 | — | — | 1 | 7.16 |
| CHEMBL51087 | — | — | 1 | 7.10 |
| CHEMBL298742 | — | — | 1 | 7.10 |
| CHEMBL300506 | — | — | 1 | 7.10 |
| CHEMBL54032 | — | — | 1 | 7.05 |
| CHEMBL50855 | — | — | 1 | 7.05 |
| CHEMBL33780 | — | — | 1 | 7.05 |
| CHEMBL49993 | — | — | 1 | 6.70 |
| CHEMBL51062 | — | — | 1 | 6.60 |
| CHEMBL301542 | — | — | 1 | 6.50 |
| CHEMBL53942 | — | — | 1 | 6.31 |
| CHEMBL300293 | — | — | 1 | 6.30 |
| CHEMBL51000 | — | — | 1 | 6.30 |
| CHEMBL50528 | — | — | 1 | 6.19 |
| CHEMBL53590 | — | — | 1 | 6.18 |
| CHEMBL52911 | — | — | 1 | 6.15 |
| CHEMBL53613 | — | — | 1 | 6.08 |
| CHEMBL299732 | — | — | 1 | 6.06 |
| CHEMBL51827 | — | — | 1 | 6.02 |
| CHEMBL274185 | LECIMIBIDE | 2.0 | 1 | 6.00 |
| CHEMBL299338 | — | — | 1 | 6.00 |
| CHEMBL299525 | — | — | 1 | 5.49 |
| CHEMBL50427 | — | — | 1 | 5.44 |
| CHEMBL299148 | — | — | 1 | 5.30 |
| CHEMBL51615 | — | — | 1 | 5.23 |
| CHEMBL50132 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53728 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL52006 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL50131 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL53397 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL54217 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL51087 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL298742 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL300506 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL54032 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL50855 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL33780 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL49993 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL51062 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL301542 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL53942 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL51000 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL300293 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL50528 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL53590 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL52911 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL53613 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL299732 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL51827 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL299338 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL274185 | LECIMIBIDE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL299525 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL50427 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL299148 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL51615 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL50132 | — | IC50 | = | 6920.0 | nM | 5.16 |
| CHEMBL51768 | — | IC50 | = | 7510.0 | nM | 5.12 |
| CHEMBL51088 | — | IC50 | = | 8330.0 | nM | 5.08 |
| CHEMBL50359 | — | IC50 | = | 55700.0 | nM | 4.25 |