Assay Detail
Functional
CHEMBL2379958
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Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.02 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376666 | — | — | 1 | 8.40 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 7.89 |
| CHEMBL2376665 | — | — | 1 | 7.80 |
| CHEMBL2376662 | — | — | 1 | 7.77 |
| CHEMBL2376663 | — | — | 1 | 7.75 |
| CHEMBL2375372 | — | — | 1 | 7.64 |
| CHEMBL2376664 | — | — | 1 | 7.55 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.51 |
| CHEMBL2376660 | — | — | 1 | 7.46 |
| CHEMBL2376667 | — | — | 1 | 7.43 |
| CHEMBL2376673 | — | — | 1 | 7.40 |
| CHEMBL2376684 | — | — | 1 | 7.30 |
| CHEMBL2376675 | — | — | 1 | 7.01 |
| CHEMBL2376676 | — | — | 1 | 6.91 |
| CHEMBL2376682 | — | — | 1 | 6.85 |
| CHEMBL2376668 | — | — | 1 | 6.83 |
| CHEMBL2376674 | — | — | 1 | 6.82 |
| CHEMBL2376680 | — | — | 1 | 6.76 |
| CHEMBL2376686 | — | — | 1 | 6.72 |
| CHEMBL2376683 | — | — | 1 | 6.66 |
| CHEMBL2376672 | — | — | 1 | 6.62 |
| CHEMBL2376670 | — | — | 1 | 6.62 |
| CHEMBL2376678 | — | — | 1 | 6.49 |
| CHEMBL2376671 | — | — | 1 | 6.46 |
| CHEMBL2376669 | — | — | 1 | 6.45 |
| CHEMBL2376681 | — | — | 1 | 6.39 |
| CHEMBL2376685 | — | — | 1 | 6.09 |
| CHEMBL2376677 | — | — | 1 | 6.01 |
| CHEMBL2376679 | — | — | 1 | 5.95 |
| CHEMBL2376661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376666 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376665 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2376662 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2376663 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2375372 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2376664 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2376660 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2376667 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2376673 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2376684 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2376675 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2376676 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2376682 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL2376668 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL2376674 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL2376680 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL2376686 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL2376683 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL2376672 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2376670 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2376678 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL2376671 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2376669 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL2376681 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL2376685 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL2376677 | — | IC50 | = | 973.0 | nM | 6.01 |
| CHEMBL2376679 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL2376661 | — | IC50 | < | 30.0 | nM | - |