Assay Detail
Functional
CHEMBL4220449
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Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COLO 205 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.83 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228425 | — | — | 1 | 8.60 |
| CHEMBL4229260 | — | — | 1 | 8.54 |
| CHEMBL4228999 | — | — | 1 | 8.33 |
| CHEMBL4225401 | — | — | 1 | 8.14 |
| CHEMBL4225654 | — | — | 1 | 8.00 |
| CHEMBL4228161 | — | — | 1 | 7.92 |
| CHEMBL4225180 | — | — | 1 | 7.42 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.23 |
| CHEMBL4225400 | — | — | 1 | 7.12 |
| CHEMBL4226300 | — | — | 1 | 7.04 |
| CHEMBL4227816 | — | — | 1 | - |
| CHEMBL4226967 | — | — | 1 | - |
| CHEMBL4227199 | — | — | 1 | - |
| CHEMBL4228687 | — | — | 1 | - |
| CHEMBL4224923 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228425 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4229260 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4228999 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4225401 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4225654 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4228161 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4225180 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4225400 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL4226300 | — | IC50 | = | 90.1 | nM | 7.04 |
| CHEMBL4227816 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4226967 | — | IC50 | - | — | - | |
| CHEMBL4227199 | — | IC50 | - | — | - | |
| CHEMBL4228687 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4224923 | — | IC50 | > | 1000.0 | nM | - |