Assay Detail
Binding
CHEMBL681806
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Inhibition of [3H]FPP incorporation into biotinylated lamin B peptide by farnesyl transferase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.51 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289228 | TIPIFARNIB | 3.0 | 1 | 9.05 |
| CHEMBL342827 | — | — | 1 | 9.00 |
| CHEMBL136831 | — | — | 1 | 8.89 |
| CHEMBL343172 | — | — | 1 | 8.77 |
| CHEMBL342254 | — | — | 1 | 8.52 |
| CHEMBL344703 | — | — | 1 | 8.40 |
| CHEMBL137087 | — | — | 1 | 8.40 |
| CHEMBL137741 | — | — | 1 | 8.30 |
| CHEMBL344642 | — | — | 1 | 8.22 |
| CHEMBL422815 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289228 | TIPIFARNIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL342827 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL136831 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL343172 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL342254 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL344703 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL137087 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL137741 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL344642 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL422815 | — | IC50 | = | 26.0 | nM | 7.58 |