Assay Detail
Binding
CHEMBL679602
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Inhibition of [3H]FPP incorporation into Ha-Ras by Farnesyltransferase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.06 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27141 | — | — | 1 | 9.00 |
| CHEMBL27486 | — | — | 1 | 9.00 |
| CHEMBL275378 | — | — | 1 | 8.52 |
| CHEMBL283208 | — | — | 1 | 8.30 |
| CHEMBL282379 | — | — | 1 | 7.62 |
| CHEMBL284424 | — | — | 1 | 7.17 |
| CHEMBL283697 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27141 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL27486 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL275378 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL283208 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL282379 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL284424 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL283697 | — | IC50 | = | 160.0 | nM | 6.80 |