Assay Detail
Binding
CHEMBL4687984
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H] cholesteryl oleate or [3H] triolein between exogenous LDL and HDL in 2% human serum
22
Total Activities
22
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
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 | 6.81 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4797108 | — | — | 1 | 7.77 |
| CHEMBL4781837 | — | — | 1 | 7.75 |
| CHEMBL4755391 | — | — | 1 | 7.55 |
| CHEMBL4763753 | — | — | 1 | 7.43 |
| CHEMBL4756571 | — | — | 1 | 7.42 |
| CHEMBL4764014 | — | — | 1 | 7.26 |
| CHEMBL4756749 | — | — | 1 | 7.02 |
| CHEMBL4755148 | — | — | 1 | 6.98 |
| CHEMBL4796671 | — | — | 1 | 6.97 |
| CHEMBL4776253 | — | — | 1 | 6.94 |
| CHEMBL4776914 | — | — | 1 | 6.87 |
| CHEMBL4748881 | — | — | 1 | 6.82 |
| CHEMBL4754631 | — | — | 1 | 6.61 |
| CHEMBL4743423 | — | — | 1 | 6.42 |
| CHEMBL4751074 | — | — | 1 | 6.41 |
| CHEMBL4795898 | — | — | 1 | 6.38 |
| CHEMBL4752734 | — | — | 1 | 6.33 |
| CHEMBL4788299 | — | — | 1 | 6.26 |
| CHEMBL4793274 | — | — | 1 | 6.26 |
| CHEMBL4760994 | — | — | 1 | 5.95 |
| CHEMBL4754455 | — | — | 1 | 5.56 |
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4797108 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4781837 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4755391 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4763753 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4756571 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4764014 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4756749 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4755148 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4796671 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4776253 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4776914 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4748881 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4754631 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4743423 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL4751074 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL4795898 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL4752734 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL4788299 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4793274 | — | IC50 | = | 544.0 | nM | 6.26 |
| CHEMBL4760994 | — | IC50 | = | 1112.0 | nM | 5.95 |
| CHEMBL4754455 | — | IC50 | = | 2779.0 | nM | 5.56 |
| CHEMBL1800807 | ANACETRAPIB | IC50 | - | — | - |