Assay Detail
Binding
CHEMBL4843592
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 [3H]LDL in 95% human serum by liquid scintillation analysis
49
Total Activities
49
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 | 49 | 6.91 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4875851 | — | — | 1 | 7.90 |
| CHEMBL4852781 | — | — | 1 | 7.75 |
| CHEMBL4876430 | — | — | 1 | 7.72 |
| CHEMBL4852134 | — | — | 1 | 7.70 |
| CHEMBL3657496 | — | — | 1 | 7.66 |
| CHEMBL4853626 | — | — | 1 | 7.64 |
| CHEMBL1800622 | — | — | 1 | 7.60 |
| CHEMBL4856008 | — | — | 1 | 7.60 |
| CHEMBL4854376 | — | — | 1 | 7.52 |
| CHEMBL4852538 | — | — | 1 | 7.47 |
| CHEMBL4848688 | — | — | 1 | 7.38 |
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | 7.35 |
| CHEMBL4846106 | — | — | 1 | 7.34 |
| CHEMBL4851648 | — | — | 1 | 7.31 |
| CHEMBL4855182 | — | — | 1 | 7.29 |
| CHEMBL4867412 | — | — | 1 | 7.27 |
| CHEMBL4870761 | — | — | 1 | 7.26 |
| CHEMBL3657493 | — | — | 1 | 7.25 |
| CHEMBL4864055 | — | — | 1 | 7.16 |
| CHEMBL3657494 | — | — | 1 | 7.15 |
| CHEMBL4878757 | — | — | 1 | 7.09 |
| CHEMBL4864315 | — | — | 1 | 7.08 |
| CHEMBL3657471 | — | — | 1 | 7.07 |
| CHEMBL4872545 | — | — | 1 | 7.03 |
| CHEMBL4850473 | — | — | 1 | 7.01 |
| CHEMBL3657499 | — | — | 1 | 6.97 |
| CHEMBL4860733 | — | — | 1 | 6.95 |
| CHEMBL4864066 | — | — | 1 | 6.88 |
| CHEMBL4874956 | — | — | 1 | 6.87 |
| CHEMBL4860491 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4875851 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4852781 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4876430 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4852134 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3657496 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4853626 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1800622 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4856008 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4854376 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4852538 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4848688 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1800807 | ANACETRAPIB | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4846106 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4851648 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4855182 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4867412 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4870761 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3657493 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4864055 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3657494 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4878757 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4864315 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3657471 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4872545 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4850473 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3657499 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4860733 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4864066 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4874956 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4860491 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4855936 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL3657498 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4850005 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4862077 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4862151 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3657497 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4847619 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL3657503 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4776253 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4849128 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL4864329 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL4756749 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3657506 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3657507 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4861223 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4862493 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4863737 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4851754 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4871886 | — | IC50 | > | 10000.0 | nM | - |