Assay Detail
Binding
CHEMBL4031871
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Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method
19
Total Activities
17
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 Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.73 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL479527 | TORCETRAPIB | 3.0 | 1 | 7.75 |
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | 7.75 |
| CHEMBL4064793 | — | — | 1 | 7.22 |
| CHEMBL4063323 | — | — | 2 | 7.22 |
| CHEMBL4075773 | — | — | 1 | 7.21 |
| CHEMBL4070653 | — | — | 1 | 7.15 |
| CHEMBL4081265 | — | — | 2 | 7.11 |
| CHEMBL2017179 | EVACETRAPIB | 3.0 | 1 | 6.96 |
| CHEMBL4103344 | — | — | 1 | 6.82 |
| CHEMBL4083767 | — | — | 1 | 6.70 |
| CHEMBL4089133 | — | — | 1 | 6.62 |
| CHEMBL4074770 | — | — | 1 | 6.29 |
| CHEMBL4064327 | — | — | 1 | 6.11 |
| CHEMBL4099797 | — | — | 1 | 5.89 |
| CHEMBL313006 | DALCETRAPIB | 3.0 | 1 | 5.39 |
| CHEMBL4060947 | — | — | 1 | 5.32 |
| CHEMBL4099285 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL479527 | TORCETRAPIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1800807 | ANACETRAPIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4064793 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4063323 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4075773 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4070653 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4081265 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL2017179 | EVACETRAPIB | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4103344 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4081265 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4063323 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4083767 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4089133 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4074770 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4064327 | — | IC50 | = | 771.0 | nM | 6.11 |
| CHEMBL4099797 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL313006 | DALCETRAPIB | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4060947 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4099285 | — | IC50 | > | 10000.0 | nM | - |