Assay Detail
Binding
CHEMBL681807
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Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyl transferase
11
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.45 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341586 | — | — | 3 | 9.22 |
| CHEMBL289228 | TIPIFARNIB | 3.0 | 1 | 9.05 |
| CHEMBL343998 | — | — | 1 | 8.82 |
| CHEMBL337751 | — | — | 3 | 8.77 |
| CHEMBL140139 | — | — | 1 | 8.52 |
| CHEMBL136633 | — | — | 1 | 8.30 |
| CHEMBL335609 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341586 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL289228 | TIPIFARNIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL343998 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL337751 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL341586 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL140139 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL337751 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL136633 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL335609 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL341586 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL337751 | — | IC50 | = | 36.0 | nM | 7.44 |