Assay Detail
Binding
CHEMBL4366085
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Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.64 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439823 | — | — | 1 | 9.00 |
| CHEMBL4574163 | — | — | 1 | 8.70 |
| CHEMBL4457286 | — | — | 1 | 8.52 |
| CHEMBL4552555 | — | — | 1 | 8.30 |
| CHEMBL4469874 | — | — | 1 | 8.30 |
| CHEMBL4439856 | — | — | 1 | 8.22 |
| CHEMBL4473304 | — | — | 1 | 7.96 |
| CHEMBL479527 | TORCETRAPIB | 3.0 | 1 | 7.92 |
| CHEMBL4468692 | — | — | 1 | 7.58 |
| CHEMBL4475826 | — | — | 1 | 7.46 |
| CHEMBL4448253 | — | — | 2 | 7.28 |
| CHEMBL4436115 | — | — | 1 | 6.92 |
| CHEMBL4545593 | — | — | 1 | 6.85 |
| CHEMBL4452514 | — | — | 1 | 6.64 |
| CHEMBL4468680 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439823 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4574163 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4457286 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4552555 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4469874 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4439856 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4473304 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL479527 | TORCETRAPIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4468692 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4475826 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4448253 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4448253 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4436115 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4545593 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4452514 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4468680 | — | IC50 | = | 3300.0 | nM | 5.48 |