Assay Detail
Binding
CHEMBL3750088
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1 (unknown origin) using biotinylated ERK1 as substrate incubated for 2 hrs by fluorescence analysis
33
Total Activities
33
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 |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.29 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3747294 | — | — | 1 | 8.00 |
| CHEMBL3746569 | — | — | 1 | 7.96 |
| CHEMBL3747066 | — | — | 1 | 7.92 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 7.89 |
| CHEMBL3746736 | — | — | 1 | 7.89 |
| CHEMBL2376666 | — | — | 1 | 7.85 |
| CHEMBL3747047 | — | — | 1 | 7.85 |
| CHEMBL3746559 | — | — | 1 | 7.85 |
| CHEMBL3747136 | — | — | 1 | 7.82 |
| CHEMBL3746467 | — | — | 1 | 7.82 |
| CHEMBL3747256 | — | — | 1 | 7.82 |
| CHEMBL3747359 | — | — | 1 | 7.75 |
| CHEMBL3746640 | — | — | 1 | 7.68 |
| CHEMBL2376663 | — | — | 1 | 7.68 |
| CHEMBL3746031 | — | — | 1 | 7.66 |
| CHEMBL3746103 | — | — | 1 | 7.55 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.51 |
| CHEMBL2376667 | — | — | 1 | 7.50 |
| CHEMBL3746537 | — | — | 1 | 7.50 |
| CHEMBL3746923 | — | — | 1 | 7.43 |
| CHEMBL3746142 | — | — | 1 | 7.09 |
| CHEMBL3747516 | — | — | 1 | 7.08 |
| CHEMBL3747368 | — | — | 1 | 7.03 |
| CHEMBL3746158 | — | — | 1 | 6.97 |
| CHEMBL3746516 | — | — | 1 | 6.93 |
| CHEMBL3746203 | — | — | 1 | 6.90 |
| CHEMBL3747610 | — | — | 1 | 6.58 |
| CHEMBL3745994 | — | — | 1 | 6.46 |
| CHEMBL3747708 | — | — | 1 | 6.42 |
| CHEMBL3747637 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3747294 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3746569 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3747066 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3746736 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376666 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3747047 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3746559 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3747136 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3746467 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3747256 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3747359 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3746640 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2376663 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3746031 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3746103 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2376667 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3746537 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3746923 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3746142 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3747516 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3747368 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3746158 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3746516 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3746203 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3747610 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL3745994 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL3747708 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL3747637 | — | IC50 | = | 592.0 | nM | 6.23 |
| CHEMBL3747496 | — | IC50 | = | 899.0 | nM | 6.05 |
| CHEMBL3746690 | — | IC50 | = | 941.0 | nM | 6.03 |
| CHEMBL3746213 | — | IC50 | = | 1900.0 | nM | 5.72 |