Assay Detail
Functional
CHEMBL3750090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation
23
Total Activities
23
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 2: Taming the sulfamide group balances compound distribution properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.62 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3747047 | — | — | 1 | 8.70 |
| CHEMBL3747256 | — | — | 1 | 8.05 |
| CHEMBL3747294 | — | — | 1 | 7.38 |
| CHEMBL3746736 | — | — | 1 | 7.30 |
| CHEMBL3747066 | — | — | 1 | 7.19 |
| CHEMBL3746467 | — | — | 1 | 7.09 |
| CHEMBL3747359 | — | — | 1 | 7.06 |
| CHEMBL3746640 | — | — | 1 | 6.91 |
| CHEMBL3746537 | — | — | 1 | 6.82 |
| CHEMBL2376663 | — | — | 1 | 6.81 |
| CHEMBL2376666 | — | — | 1 | 6.75 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 6.73 |
| CHEMBL3746559 | — | — | 1 | 6.56 |
| CHEMBL3747136 | — | — | 1 | 6.54 |
| CHEMBL3746031 | — | — | 1 | 6.52 |
| CHEMBL3747516 | — | — | 1 | 6.14 |
| CHEMBL3746923 | — | — | 1 | 6.12 |
| CHEMBL3746569 | — | — | 1 | 5.75 |
| CHEMBL3746142 | — | — | 1 | 5.62 |
| CHEMBL3747368 | — | — | 1 | 5.60 |
| CHEMBL3746103 | — | — | 1 | 5.53 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 5.52 |
| CHEMBL2376667 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3747047 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3747256 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3747294 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3746736 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3747066 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3746467 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3747359 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3746640 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3746537 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL2376663 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2376666 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3746559 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL3747136 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL3746031 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL3747516 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL3746923 | — | IC50 | = | 757.0 | nM | 6.12 |
| CHEMBL3746569 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3746142 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3747368 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL3746103 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2376667 | — | IC50 | = | 3500.0 | nM | 5.46 |