Assay Detail
Functional
CHEMBL2379957
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Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| 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 | 20 | 5.90 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2376665 | — | — | 1 | 6.99 |
| CHEMBL2376663 | — | — | 1 | 6.81 |
| CHEMBL2376666 | — | — | 1 | 6.75 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 6.71 |
| CHEMBL2376661 | — | — | 1 | 6.54 |
| CHEMBL2376664 | — | — | 1 | 6.38 |
| CHEMBL2376662 | — | — | 1 | 6.34 |
| CHEMBL2376675 | — | — | 1 | 5.90 |
| CHEMBL2376674 | — | — | 1 | 5.68 |
| CHEMBL2376684 | — | — | 1 | 5.64 |
| CHEMBL2376673 | — | — | 1 | 5.61 |
| CHEMBL2376680 | — | — | 1 | 5.52 |
| CHEMBL2376676 | — | — | 1 | 5.52 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 5.51 |
| CHEMBL2376668 | — | — | 1 | 5.47 |
| CHEMBL2376667 | — | — | 1 | 5.46 |
| CHEMBL2375372 | — | — | 1 | 5.42 |
| CHEMBL2376682 | — | — | 1 | 5.38 |
| CHEMBL2376660 | — | — | 1 | 5.35 |
| CHEMBL2376686 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2376665 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2376663 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2376666 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL2376661 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL2376664 | — | IC50 | = | 412.0 | nM | 6.38 |
| CHEMBL2376662 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL2376675 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL2376674 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL2376684 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL2376673 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL2376680 | — | IC50 | = | 3040.0 | nM | 5.52 |
| CHEMBL2376676 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2376668 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2376667 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL2375372 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2376682 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL2376660 | — | IC50 | = | 4510.0 | nM | 5.35 |
| CHEMBL2376686 | — | IC50 | = | 8810.0 | nM | 5.05 |