Assay Detail
Binding
CHEMBL5157583
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Inhibition of KRAS G12C mutant (unknown origin) assessed as inhibition of SOS1-catalyzed nucleotide exchange measured by HTRF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 | 6 | 6.99 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | 4.0 | 1 | 8.02 |
| CHEMBL5171974 | — | — | 1 | 7.59 |
| CHEMBL5206068 | — | — | 1 | 7.02 |
| CHEMBL5205064 | — | — | 1 | 6.57 |
| CHEMBL5194712 | — | — | 1 | 6.55 |
| CHEMBL5185805 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | IC50 | = | 9.66 | nM | 8.02 |
| CHEMBL5171974 | — | IC50 | = | 25.44 | nM | 7.59 |
| CHEMBL5206068 | — | IC50 | = | 96.32 | nM | 7.02 |
| CHEMBL5205064 | — | IC50 | = | 270.88 | nM | 6.57 |
| CHEMBL5194712 | — | IC50 | = | 283.84 | nM | 6.55 |
| CHEMBL5185805 | — | IC50 | = | 639.91 | nM | 6.19 |