Assay Detail
Functional
CHEMBL4199966
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Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.96 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205192 | — | — | 1 | 7.31 |
| CHEMBL4213970 | MK-8353 | 1.0 | 1 | 7.29 |
| CHEMBL3590107 | — | — | 1 | 7.23 |
| CHEMBL4206960 | — | — | 1 | 7.22 |
| CHEMBL4218701 | — | — | 1 | 7.11 |
| CHEMBL4209049 | — | — | 1 | 7.10 |
| CHEMBL4209570 | — | — | 1 | 7.10 |
| CHEMBL4215228 | — | — | 1 | 7.06 |
| CHEMBL4204707 | — | — | 1 | 7.00 |
| CHEMBL3645235 | — | — | 1 | 6.93 |
| CHEMBL4216900 | — | — | 1 | 6.88 |
| CHEMBL4216709 | — | — | 1 | 6.68 |
| CHEMBL4211744 | — | — | 1 | 6.61 |
| CHEMBL4218370 | — | — | 1 | 6.61 |
| CHEMBL4207383 | — | — | 1 | 6.26 |
| CHEMBL4212273 | — | — | 1 | - |
| CHEMBL4203551 | — | — | 1 | - |
| CHEMBL4213444 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205192 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4213970 | MK-8353 | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3590107 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4206960 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4218701 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4209049 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4209570 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4215228 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4204707 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3645235 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4216900 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4216709 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL4211744 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL4218370 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4207383 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL4212273 | — | IC50 | - | — | - | |
| CHEMBL4203551 | — | IC50 | - | — | - | |
| CHEMBL4213444 | — | IC50 | - | — | - |