Assay Detail
ADMET
CHEMBL4199969
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Inhibition of CYP3A4 (unknown origin) preincubated followed by substrate addition
4
Total Activities
4
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 |
Publication
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.15 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218701 | — | — | 1 | 6.52 |
| CHEMBL4213970 | MK-8353 | 1.0 | 1 | 5.77 |
| CHEMBL3590107 | — | — | 1 | - |
| CHEMBL3645235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218701 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4213970 | MK-8353 | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3590107 | — | IC50 | = | 5700000.0 | nM | - |
| CHEMBL3645235 | — | IC50 | = | 2000000.0 | nM | - |