Assay Detail
Binding
CHEMBL680439
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In vitro inhibitory activity against farnesyltransferase (FTase)
22
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.28 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282959 | — | — | 1 | 9.43 |
| CHEMBL27843 | — | — | 1 | 9.41 |
| CHEMBL431884 | — | — | 1 | 9.35 |
| CHEMBL289228 | TIPIFARNIB | 3.0 | 1 | 9.24 |
| CHEMBL28707 | — | — | 1 | 9.01 |
| CHEMBL29982 | — | — | 1 | 9.00 |
| CHEMBL28252 | — | — | 2 | 8.82 |
| CHEMBL29645 | — | — | 2 | 8.82 |
| CHEMBL28770 | — | — | 1 | 8.82 |
| CHEMBL29064 | — | — | 2 | 8.72 |
| CHEMBL28970 | — | — | 1 | 8.72 |
| CHEMBL298734 | LONAFARNIB | 4.0 | 1 | 8.11 |
| CHEMBL284448 | — | — | 1 | 8.00 |
| CHEMBL28659 | — | — | 1 | 7.96 |
| CHEMBL28588 | — | — | 1 | 7.85 |
| CHEMBL28490 | — | — | 1 | 7.75 |
| CHEMBL28937 | — | — | 1 | 7.19 |
| CHEMBL282368 | — | — | 1 | 7.08 |
| CHEMBL27750 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282959 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL27843 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL431884 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL289228 | TIPIFARNIB | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL28707 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL29982 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL28252 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL29645 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL28770 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL29064 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL28970 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL298734 | LONAFARNIB | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL284448 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL29645 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL28659 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL28588 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL28490 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL29064 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL28252 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL28937 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL282368 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL27750 | — | IC50 | = | 1000.0 | nM | 6.00 |