Assay Detail
Functional
CHEMBL5157585
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Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H23 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Efficient targeted oncogenic KRAS<sup>G12C</sup> degradation via first reversible-covalent PROTAC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.67 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | 4.0 | 1 | 6.95 |
| CHEMBL5183098 | — | — | 1 | 6.61 |
| CHEMBL5194712 | — | — | 1 | 5.50 |
| CHEMBL5171974 | — | — | 1 | 5.28 |
| CHEMBL5185805 | — | — | 1 | 5.20 |
| CHEMBL5205064 | — | — | 1 | 5.13 |
| CHEMBL5206068 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | IC50 | = | 111.5 | nM | 6.95 |
| CHEMBL5183098 | — | IC50 | = | 243.9 | nM | 6.61 |
| CHEMBL5194712 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL5171974 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL5185805 | — | IC50 | = | 6330.0 | nM | 5.20 |
| CHEMBL5205064 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5206068 | — | IC50 | = | 9550.0 | nM | 5.02 |