Assay Detail
Binding
CHEMBL4687985
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Inhibition of CETP in 95% human serum assessed as inhibition of transfer of [3H] cholesteryl oleate or [3H] triolein between LDL and HDL
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Serum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.22 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | 7.28 |
| CHEMBL4764014 | — | — | 1 | 7.02 |
| CHEMBL4755391 | — | — | 1 | 6.89 |
| CHEMBL4796671 | — | — | 1 | 6.52 |
| CHEMBL4763753 | — | — | 1 | 6.47 |
| CHEMBL4797108 | — | — | 1 | 6.44 |
| CHEMBL4755148 | — | — | 1 | 6.41 |
| CHEMBL4756571 | — | — | 1 | 6.40 |
| CHEMBL4781837 | — | — | 1 | 6.35 |
| CHEMBL4776253 | — | — | 1 | 6.32 |
| CHEMBL4756749 | — | — | 1 | 6.15 |
| CHEMBL4748881 | — | — | 1 | 6.10 |
| CHEMBL4776914 | — | — | 1 | 6.01 |
| CHEMBL4788299 | — | — | 1 | 5.92 |
| CHEMBL4743423 | — | — | 1 | 5.87 |
| CHEMBL4795898 | — | — | 1 | 5.85 |
| CHEMBL4754631 | — | — | 1 | 5.82 |
| CHEMBL4793274 | — | — | 1 | 5.80 |
| CHEMBL4760994 | — | — | 1 | 5.76 |
| CHEMBL4752734 | — | — | 1 | 5.71 |
| CHEMBL4751074 | — | — | 1 | 5.57 |
| CHEMBL4754455 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800807 | ANACETRAPIB | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4764014 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4755391 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4796671 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4763753 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL4797108 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL4755148 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4756571 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL4781837 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL4776253 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL4756749 | — | IC50 | = | 701.0 | nM | 6.15 |
| CHEMBL4748881 | — | IC50 | = | 795.0 | nM | 6.10 |
| CHEMBL4776914 | — | IC50 | = | 984.0 | nM | 6.01 |
| CHEMBL4788299 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4743423 | — | IC50 | = | 1362.0 | nM | 5.87 |
| CHEMBL4795898 | — | IC50 | = | 1419.0 | nM | 5.85 |
| CHEMBL4754631 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4793274 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL4760994 | — | IC50 | = | 1727.0 | nM | 5.76 |
| CHEMBL4752734 | — | IC50 | = | 1934.0 | nM | 5.71 |
| CHEMBL4751074 | — | IC50 | = | 2684.0 | nM | 5.57 |
| CHEMBL4754455 | — | IC50 | > | 10000.0 | nM | - |