Assay Detail
Functional
CHEMBL5157586
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Antiproliferative activity against human A549 cells harboring KRAS G12S 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 | A549 |
| 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 | 4.66 | 5.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206068 | — | — | 1 | 5.09 |
| CHEMBL5171974 | — | — | 1 | 4.88 |
| CHEMBL5185805 | — | — | 1 | 4.79 |
| CHEMBL5205064 | — | — | 1 | 4.60 |
| CHEMBL4535757 | SOTORASIB | 4.0 | 1 | 4.30 |
| CHEMBL5194712 | — | — | 1 | 4.30 |
| CHEMBL5183098 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206068 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL5171974 | — | IC50 | = | 13270.0 | nM | 4.88 |
| CHEMBL5185805 | — | IC50 | = | 16140.0 | nM | 4.79 |
| CHEMBL5205064 | — | IC50 | = | 25320.0 | nM | 4.60 |
| CHEMBL4535757 | SOTORASIB | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5194712 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5183098 | — | IC50 | - | — | - |