Assay Detail
Binding
CHEMBL831437
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inhibitory concentration needed to to reduce the bovine GGTase-catalyzed incorporation of [3H]-FPP into a biotin-linked K-ras (B) decapeptide
13
Total Activities
13
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
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.08 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL158553 | — | — | 1 | 8.89 |
| CHEMBL128309 | — | — | 1 | 8.57 |
| CHEMBL363518 | — | — | 1 | 5.92 |
| CHEMBL365269 | — | — | 1 | 5.72 |
| CHEMBL183265 | — | — | 1 | 5.70 |
| CHEMBL183087 | — | — | 1 | 5.44 |
| CHEMBL184805 | — | — | 1 | 5.21 |
| CHEMBL185202 | — | — | 1 | 5.18 |
| CHEMBL425539 | — | — | 1 | 5.11 |
| CHEMBL365718 | — | — | 1 | 5.03 |
| CHEMBL185492 | — | — | 1 | - |
| CHEMBL184169 | — | — | 1 | - |
| CHEMBL365300 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL158553 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL128309 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL363518 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL365269 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL183265 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL183087 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL184805 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL185202 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL425539 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL365718 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL185492 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL184169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL365300 | — | IC50 | > | 10000.0 | nM | - |