Assay Detail
Binding
CHEMBL828420
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]FPP incorporation into H-ras CVLS by Farnesyltransferase
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.77 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186303 | — | — | 1 | 9.49 |
| CHEMBL364342 | — | — | 1 | 9.40 |
| CHEMBL298734 | LONAFARNIB | 4.0 | 1 | 8.70 |
| CHEMBL365463 | — | — | 1 | 8.48 |
| CHEMBL359779 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186303 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL364342 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL298734 | LONAFARNIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL365463 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL359779 | — | IC50 | = | 16.0 | nM | 7.80 |