Assay Detail
Binding
CHEMBL4620552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GFP-tagged KRAS G12V mutant (unknown origin) expressed in MDCK cells cotransfected with mCherry-CAXX assessed as increase in KRAS G12V-plasma membrane dissociation incubated for 48 hrs by quantitative confocal microscopic method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.94 | 5.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL598038 | — | — | 1 | 5.15 |
| CHEMBL62070 | — | — | 1 | 5.13 |
| CHEMBL4646677 | — | — | 1 | 5.13 |
| CHEMBL4643559 | — | — | 1 | 5.09 |
| CHEMBL59351 | — | — | 1 | 5.09 |
| CHEMBL187437 | — | — | 1 | 5.08 |
| CHEMBL471655 | — | — | 1 | 5.04 |
| CHEMBL59026 | — | — | 1 | 4.80 |
| CHEMBL589993 | — | — | 1 | 4.61 |
| CHEMBL3219765 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL598038 | — | IC50 | = | 7010.0 | nM | 5.15 |
| CHEMBL62070 | — | IC50 | = | 7420.0 | nM | 5.13 |
| CHEMBL4646677 | — | IC50 | = | 7490.0 | nM | 5.13 |
| CHEMBL4643559 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL59351 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL187437 | — | IC50 | = | 8290.0 | nM | 5.08 |
| CHEMBL471655 | — | IC50 | = | 9170.0 | nM | 5.04 |
| CHEMBL59026 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL589993 | — | IC50 | = | 24640.0 | nM | 4.61 |
| CHEMBL3219765 | — | IC50 | = | 52970.0 | nM | 4.28 |