Assay Detail
Functional
CHEMBL5217982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H358 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS<sup>G12C</sup> Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.89 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | 4.0 | 1 | 8.19 |
| CHEMBL5218642 | — | — | 1 | 7.58 |
| CHEMBL5219918 | — | — | 1 | - |
| CHEMBL5218841 | — | — | 1 | - |
| CHEMBL5221087 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4535757 | SOTORASIB | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5218642 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5219918 | — | EC50 | - | — | - | |
| CHEMBL5218841 | — | EC50 | - | — | - | |
| CHEMBL5221087 | — | EC50 | - | — | - |