Assay Detail
Binding
CHEMBL832946
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Inhibition of [3H]FPP incorporation into biotin-linked K-ras decapeptide (CVIM) by bovine farnesyltransferase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.57 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL128309 | — | — | 1 | 9.36 |
| CHEMBL158553 | — | — | 1 | 9.06 |
| CHEMBL365718 | — | — | 1 | 8.96 |
| CHEMBL185492 | — | — | 1 | 8.92 |
| CHEMBL365269 | — | — | 1 | 8.89 |
| CHEMBL363518 | — | — | 1 | 8.68 |
| CHEMBL183265 | — | — | 1 | 8.68 |
| CHEMBL425539 | — | — | 1 | 8.64 |
| CHEMBL185202 | — | — | 1 | 8.52 |
| CHEMBL183087 | — | — | 1 | 8.12 |
| CHEMBL184805 | — | — | 1 | 7.96 |
| CHEMBL184169 | — | — | 1 | 7.92 |
| CHEMBL365300 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL128309 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL158553 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL365718 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL185492 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL365269 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL363518 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL183265 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL425539 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL185202 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL183087 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL184805 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL184169 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL365300 | — | IC50 | = | 19.0 | nM | 7.72 |