Assay Detail
Binding
CHEMBL4843620
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 using exogenous LDL and HDL in 2% human serum by liquid scintillation analysis
10
Total Activities
10
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
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.32 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800622 | — | — | 1 | 8.15 |
| CHEMBL4873416 | — | — | 1 | 8.05 |
| CHEMBL4875851 | — | — | 1 | 7.90 |
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | 7.77 |
| CHEMBL4859118 | — | — | 1 | 7.53 |
| CHEMBL4876714 | — | — | 1 | 7.52 |
| CHEMBL4875002 | — | — | 1 | 7.38 |
| CHEMBL4858285 | — | — | 1 | 7.09 |
| CHEMBL4850728 | — | — | 1 | 6.30 |
| CHEMBL4849688 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800622 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4873416 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4875851 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL1800807 | ANACETRAPIB | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4859118 | — | IC50 | = | 29.48 | nM | 7.53 |
| CHEMBL4876714 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL4875002 | — | IC50 | = | 41.8 | nM | 7.38 |
| CHEMBL4858285 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4850728 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL4849688 | — | IC50 | = | 3060.0 | nM | 5.51 |