Assay Detail
Binding
CHEMBL4199965
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Inhibition of ERK2 (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 | 7.80 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590107 | — | — | 1 | 9.00 |
| CHEMBL4209570 | — | — | 1 | 8.77 |
| CHEMBL4205192 | — | — | 1 | 8.30 |
| CHEMBL4206960 | — | — | 1 | 8.30 |
| CHEMBL4215228 | — | — | 1 | 8.25 |
| CHEMBL4216900 | — | — | 1 | 8.22 |
| CHEMBL3645235 | — | — | 1 | 8.15 |
| CHEMBL4213970 | MK-8353 | 1.0 | 1 | 8.15 |
| CHEMBL4209049 | — | — | 1 | 7.89 |
| CHEMBL4218701 | — | — | 1 | 7.89 |
| CHEMBL4211744 | — | — | 1 | 7.64 |
| CHEMBL4216709 | — | — | 1 | 7.60 |
| CHEMBL4204707 | — | — | 1 | 7.57 |
| CHEMBL4218370 | — | — | 1 | 7.54 |
| CHEMBL4207383 | — | — | 1 | 7.44 |
| CHEMBL4203551 | — | — | 1 | 6.94 |
| CHEMBL4212273 | — | — | 1 | 6.54 |
| CHEMBL4213444 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590107 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4209570 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4205192 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4206960 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4215228 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4216900 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3645235 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4213970 | MK-8353 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4209049 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4218701 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4211744 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4216709 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4204707 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4218370 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4207383 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4203551 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4212273 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4213444 | — | IC50 | = | 729.0 | nM | 6.14 |