Assay Detail
Functional
CHEMBL3750089
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A375 cells harboring BRAF(V600E) mutation after 72 hrs by cell titer glow cell titer glow FCTGI assay
31
Total Activities
31
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 2: Taming the sulfamide group balances compound distribution properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3747047 | — | — | 1 | 9.70 |
| CHEMBL3746736 | — | — | 1 | 8.70 |
| CHEMBL3747256 | — | — | 1 | 8.70 |
| CHEMBL3747066 | — | — | 1 | 8.62 |
| CHEMBL2376666 | — | — | 1 | 8.40 |
| CHEMBL3746640 | — | — | 1 | 8.40 |
| CHEMBL3746467 | — | — | 1 | 8.40 |
| CHEMBL3747294 | — | — | 1 | 8.22 |
| CHEMBL3747359 | — | — | 1 | 8.22 |
| CHEMBL3746537 | — | — | 1 | 8.10 |
| CHEMBL3746031 | — | — | 1 | 7.96 |
| CHEMBL3746559 | — | — | 1 | 7.89 |
| CHEMBL2376663 | — | — | 1 | 7.75 |
| CHEMBL3747516 | — | — | 1 | 7.62 |
| CHEMBL3746103 | — | — | 1 | 7.50 |
| CHEMBL3746923 | — | — | 1 | 7.46 |
| CHEMBL2376667 | — | — | 1 | 7.43 |
| CHEMBL3746142 | — | — | 1 | 7.19 |
| CHEMBL3746569 | — | — | 1 | 7.06 |
| CHEMBL3747368 | — | — | 1 | 7.05 |
| CHEMBL3746158 | — | — | 1 | 6.86 |
| CHEMBL3747610 | — | — | 1 | 6.75 |
| CHEMBL3747708 | — | — | 1 | 6.66 |
| CHEMBL3746203 | — | — | 1 | 6.47 |
| CHEMBL3746516 | — | — | 1 | 6.43 |
| CHEMBL3745994 | — | — | 1 | 6.32 |
| CHEMBL3747496 | — | — | 1 | 6.24 |
| CHEMBL3747637 | — | — | 1 | 6.14 |
| CHEMBL3746690 | — | — | 1 | 6.04 |
| CHEMBL3746213 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3747047 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3746736 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3747256 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3747066 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2376666 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3746640 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3746467 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3747294 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3747359 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3746537 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3746031 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3746559 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376663 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3747516 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3746103 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3746923 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2376667 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3746142 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3746569 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3747368 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3746158 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL3747610 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3747708 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL3746203 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL3746516 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL3745994 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL3747496 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3747637 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL3746690 | — | IC50 | = | 922.0 | nM | 6.04 |
| CHEMBL3746213 | — | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL3747136 | — | IC50 | < | 30.0 | nM | - |