Assay Detail
Binding
CHEMBL682423
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Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Rat1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.53 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52073 | — | — | 1 | 9.54 |
| CHEMBL156586 | — | — | 1 | 9.52 |
| CHEMBL346700 | — | — | 1 | 9.48 |
| CHEMBL346771 | — | — | 1 | 9.36 |
| CHEMBL160223 | — | — | 1 | 9.23 |
| CHEMBL349329 | — | — | 1 | 9.07 |
| CHEMBL347018 | — | — | 1 | 9.00 |
| CHEMBL346084 | — | — | 1 | 8.96 |
| CHEMBL160204 | — | — | 1 | 8.92 |
| CHEMBL423062 | — | — | 1 | 8.85 |
| CHEMBL424338 | — | — | 1 | 8.66 |
| CHEMBL348336 | — | — | 1 | 8.48 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 8.44 |
| CHEMBL159171 | — | — | 1 | 8.24 |
| CHEMBL346589 | — | — | 1 | 8.00 |
| CHEMBL350680 | — | — | 1 | 7.70 |
| CHEMBL157295 | — | — | 1 | 7.55 |
| CHEMBL345474 | — | — | 1 | 7.52 |
| CHEMBL156225 | — | — | 1 | 7.40 |
| CHEMBL158586 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52073 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL156586 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL346700 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL346771 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL160223 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL349329 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL347018 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL346084 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL160204 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL423062 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL424338 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL348336 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL159171 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL346589 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL350680 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL157295 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL345474 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL156225 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL158586 | — | IC50 | = | 170.0 | nM | 6.77 |