Assay Detail
Binding
CHEMBL4199964
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Inhibition of ERK1 (unknown origin) using peptide substrate measured after 45 mins by IMAP assay
18
Total Activities
18
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
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.24 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209570 | — | — | 1 | 8.10 |
| CHEMBL3590107 | — | — | 1 | 8.10 |
| CHEMBL4205192 | — | — | 1 | 7.77 |
| CHEMBL4206960 | — | — | 1 | 7.72 |
| CHEMBL4213970 | MK-8353 | 1.0 | 1 | 7.70 |
| CHEMBL4215228 | — | — | 1 | 7.60 |
| CHEMBL4216900 | — | — | 1 | 7.47 |
| CHEMBL3645235 | — | — | 1 | 7.39 |
| CHEMBL4211744 | — | — | 1 | 7.37 |
| CHEMBL4218701 | — | — | 1 | 7.35 |
| CHEMBL4204707 | — | — | 1 | 7.13 |
| CHEMBL4209049 | — | — | 1 | 7.03 |
| CHEMBL4216709 | — | — | 1 | 6.87 |
| CHEMBL4207383 | — | — | 1 | 6.68 |
| CHEMBL4218370 | — | — | 1 | 6.64 |
| CHEMBL4203551 | — | — | 1 | 6.18 |
| CHEMBL4212273 | — | — | 1 | 6.02 |
| CHEMBL4213444 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209570 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3590107 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4205192 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4206960 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4213970 | MK-8353 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4215228 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4216900 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3645235 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4211744 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4218701 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4204707 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4209049 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4216709 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4207383 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4218370 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL4203551 | — | IC50 | = | 663.0 | nM | 6.18 |
| CHEMBL4212273 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL4213444 | — | IC50 | - | — | - |