Assay Detail
ADMET
CHEMBL4843602
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Transactivation of PXR (unknown origin)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| EC50 | 13 | 5.54 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4857594 | — | — | 1 | 6.52 |
| CHEMBL4846038 | — | — | 1 | 5.70 |
| CHEMBL1800622 | — | — | 1 | 5.58 |
| CHEMBL1800807 | ANACETRAPIB | 3.0 | 1 | 5.41 |
| CHEMBL4876714 | — | — | 1 | 5.12 |
| CHEMBL4868133 | — | — | 1 | 4.89 |
| CHEMBL4850728 | — | — | 1 | - |
| CHEMBL4875002 | — | — | 1 | - |
| CHEMBL4859118 | — | — | 1 | - |
| CHEMBL4849688 | — | — | 1 | - |
| CHEMBL4858285 | — | — | 1 | - |
| CHEMBL4873416 | — | — | 1 | - |
| CHEMBL4875851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4857594 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4846038 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1800622 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1800807 | ANACETRAPIB | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4876714 | — | EC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4868133 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4850728 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4875002 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4859118 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4849688 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4858285 | — | EC50 | - | — | - | |
| CHEMBL4873416 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4875851 | — | EC50 | > | 30000.0 | nM | - |