Assay Detail
Functional
CHEMBL758028
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Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PSN1 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.92 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52073 | — | — | 1 | 8.70 |
| CHEMBL349329 | — | — | 1 | 8.00 |
| CHEMBL159171 | — | — | 1 | 7.92 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52073 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL349329 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL159171 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL279433 | L-778123 FREE BASE | EC50 | = | 92.0 | nM | 7.04 |