Assay Detail
Functional
CHEMBL681286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | Rat1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.27 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 8.52 |
| CHEMBL283203 | — | — | 1 | 8.10 |
| CHEMBL30270 | — | — | 1 | 7.77 |
| CHEMBL418036 | — | — | 1 | 7.39 |
| CHEMBL31828 | — | — | 1 | 7.32 |
| CHEMBL30349 | — | — | 1 | 7.03 |
| CHEMBL31031 | — | — | 1 | 6.96 |
| CHEMBL439917 | — | — | 1 | 6.59 |
| CHEMBL30858 | — | — | 1 | 6.51 |
| CHEMBL30925 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL283203 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL30270 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL418036 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL31828 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL30349 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL31031 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL439917 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL30858 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL30925 | — | IC50 | = | 350.0 | nM | 6.46 |