Assay Detail
Functional
CHEMBL4357260
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Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MIA PaCa-2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.08 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4539214 | — | — | 1 | 9.00 |
| CHEMBL4452137 | — | — | 1 | 8.70 |
| CHEMBL4527861 | — | — | 1 | 8.52 |
| CHEMBL4578214 | — | — | 1 | 8.52 |
| CHEMBL4456801 | — | — | 1 | 8.40 |
| CHEMBL4535757 | SOTORASIB | 4.0 | 1 | 8.30 |
| CHEMBL4450519 | — | — | 1 | 8.30 |
| CHEMBL4450657 | — | — | 1 | 8.30 |
| CHEMBL4465551 | — | — | 1 | 8.22 |
| CHEMBL4441771 | — | — | 1 | 8.05 |
| CHEMBL4439782 | — | — | 1 | 7.96 |
| CHEMBL4452622 | — | — | 1 | 7.96 |
| CHEMBL4450041 | — | — | 1 | 7.89 |
| CHEMBL4449810 | — | — | 1 | 7.85 |
| CHEMBL4591772 | — | — | 1 | 7.80 |
| CHEMBL4458041 | — | — | 1 | 7.80 |
| CHEMBL4569344 | — | — | 1 | 7.77 |
| CHEMBL4454645 | — | — | 1 | 7.75 |
| CHEMBL4469638 | — | — | 1 | 7.66 |
| CHEMBL4517656 | — | — | 1 | 7.48 |
| CHEMBL4438343 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4539214 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4452137 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4527861 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4578214 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4456801 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4535757 | SOTORASIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4450519 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4450657 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4465551 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4441771 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4439782 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4452622 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4450041 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4449810 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4591772 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4458041 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4569344 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4454645 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4469638 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4517656 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4438343 | — | IC50 | = | 40.0 | nM | 7.40 |