Assay Detail
Binding
CHEMBL3593135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by RapidFire Mass Spectrometry in presence of ATP at higher concentration
19
Total Activities
19
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
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.02 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590120 | — | — | 1 | 8.52 |
| CHEMBL3590118 | — | — | 1 | 8.27 |
| CHEMBL3590121 | — | — | 1 | 8.07 |
| CHEMBL3590123 | — | — | 1 | 7.89 |
| CHEMBL3590110 | — | — | 1 | 7.77 |
| CHEMBL3590125 | — | — | 1 | 7.33 |
| CHEMBL3590117 | — | — | 1 | 7.22 |
| CHEMBL3590122 | — | — | 1 | 7.06 |
| CHEMBL3590124 | — | — | 1 | 7.05 |
| CHEMBL3590111 | — | — | 1 | 6.96 |
| CHEMBL3590109 | — | — | 1 | 6.66 |
| CHEMBL3590114 | — | — | 1 | 6.47 |
| CHEMBL3590116 | — | — | 1 | 6.42 |
| CHEMBL3590113 | — | — | 1 | 5.75 |
| CHEMBL3590108 | — | — | 1 | 5.43 |
| CHEMBL3590119 | — | — | 1 | 5.40 |
| CHEMBL3590112 | — | — | 1 | - |
| CHEMBL3590107 | — | — | 1 | - |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590120 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3590118 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3590121 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3590123 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3590110 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3590125 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3590117 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3590122 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3590124 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3590111 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3590109 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3590114 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3590116 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3590113 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3590108 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3590119 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3590112 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3590107 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | IC50 | < | 0.3 | nM | - |