Assay Detail
Binding
CHEMBL5386824
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Inhibition of KRAS G12C mutant/SOS1 (unknown origin) interaction incubated for 2 hrs in presence of GTP by HTRF assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Identification of novel Pyrrolo[2,3-d]Pyrimidine-based KRAS G12C inhibitors with anticancer effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.11 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4594350 | ADAGRASIB | 4.0 | 1 | 6.89 |
| CHEMBL5396975 | — | — | 1 | 6.68 |
| CHEMBL5436457 | — | — | 1 | 6.47 |
| CHEMBL5397869 | — | — | 1 | 5.81 |
| CHEMBL5421002 | — | — | 1 | 5.71 |
| CHEMBL5417485 | — | — | 1 | 5.69 |
| CHEMBL5396264 | — | — | 1 | 5.49 |
| CHEMBL5440390 | — | — | 1 | - |
| CHEMBL5397514 | — | — | 1 | - |
| CHEMBL5396651 | — | — | 1 | - |
| CHEMBL5423454 | — | — | 1 | - |
| CHEMBL5402796 | — | — | 1 | - |
| CHEMBL5409675 | — | — | 1 | - |
| CHEMBL5437591 | — | — | 1 | - |
| CHEMBL5433037 | — | — | 1 | - |
| CHEMBL5405829 | — | — | 1 | - |
| CHEMBL5406834 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4594350 | ADAGRASIB | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5396975 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5436457 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5397869 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL5421002 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL5417485 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL5396264 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL5440390 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5397514 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5396651 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5423454 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5402796 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5409675 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5437591 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5433037 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5405829 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406834 | — | IC50 | > | 10000.0 | nM | - |