Assay Detail
Binding
CHEMBL4329928
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Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation measured after 3 hrs by Western blot analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H358 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.02 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456598 | — | — | 1 | 7.16 |
| CHEMBL4465028 | — | — | 1 | 6.27 |
| CHEMBL4525173 | — | — | 1 | 5.82 |
| CHEMBL4550990 | — | — | 1 | 5.72 |
| CHEMBL4457300 | — | — | 1 | 5.12 |
| CHEMBL4466927 | — | — | 1 | - |
| CHEMBL4549643 | — | — | 1 | - |
| CHEMBL4453071 | — | — | 1 | - |
| CHEMBL4453012 | — | — | 1 | - |
| CHEMBL4540074 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456598 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4465028 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4525173 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4550990 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4457300 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4466927 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4549643 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4453071 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4453012 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4540074 | — | IC50 | > | 16000.0 | nM | - |