Assay Detail
Binding
CHEMBL681408
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Inhibition of the Farnesyltransferase catalyzed incorporation of [3H]FPP into recombinant Ha-Ras by 50% in bovine brain at a concentration of ca. 1 nM.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
DIARYLETHER INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.62 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25734 | — | — | 1 | 6.60 |
| CHEMBL26682 | — | — | 1 | 6.48 |
| CHEMBL26314 | — | — | 1 | 6.47 |
| CHEMBL285827 | — | — | 1 | 6.39 |
| CHEMBL26255 | — | — | 1 | 6.34 |
| CHEMBL27181 | — | — | 1 | 6.21 |
| CHEMBL26149 | — | — | 1 | 6.19 |
| CHEMBL27319 | — | — | 1 | 5.64 |
| CHEMBL26371 | — | — | 1 | 5.50 |
| CHEMBL25978 | — | — | 1 | 5.42 |
| CHEMBL27407 | — | — | 1 | 5.16 |
| CHEMBL283441 | — | — | 1 | 4.80 |
| CHEMBL418200 | — | — | 1 | 4.41 |
| CHEMBL27476 | — | — | 1 | 4.35 |
| CHEMBL27078 | — | — | 1 | 4.35 |
| CHEMBL26031 | — | — | 1 | - |
| CHEMBL26134 | — | — | 1 | - |
| CHEMBL26785 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25734 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL26682 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL26314 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL285827 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL26255 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL27181 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL26149 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL27319 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL26371 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL25978 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL27407 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL283441 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL418200 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL27476 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL27078 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL26031 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL26134 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL26785 | — | IC50 | > | 100000.0 | nM | - |