Assay Detail
Binding
CHEMBL3117844
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Inhibition of FTase (unknown origin) assessed as transfer of [H3]farnesyl from [H3]farnesyl pyrophosphate to trichloroacetic acid-precipitable HaRas-CVLS
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.97 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3115255 | — | — | 1 | 10.00 |
| CHEMBL3115256 | — | — | 1 | 10.00 |
| CHEMBL3115258 | — | — | 1 | 9.70 |
| CHEMBL601202 | — | — | 1 | 9.52 |
| CHEMBL3115265 | — | — | 1 | 9.40 |
| CHEMBL3115426 | — | — | 1 | 9.22 |
| CHEMBL3115261 | — | — | 1 | 9.22 |
| CHEMBL3115429 | — | — | 1 | 9.22 |
| CHEMBL3115266 | — | — | 1 | 9.15 |
| CHEMBL3115254 | — | — | 1 | 9.10 |
| CHEMBL3115257 | — | — | 1 | 9.05 |
| CHEMBL3115253 | — | — | 1 | 8.85 |
| CHEMBL3115427 | — | — | 1 | 8.85 |
| CHEMBL3115259 | — | — | 1 | 8.77 |
| CHEMBL3115263 | — | — | 1 | 8.74 |
| CHEMBL3115251 | — | — | 1 | 8.74 |
| CHEMBL3115248 | — | — | 1 | 8.72 |
| CHEMBL3115262 | — | — | 1 | 8.59 |
| CHEMBL3115431 | — | — | 1 | 8.49 |
| CHEMBL3115430 | — | — | 1 | 8.49 |
| CHEMBL3115252 | — | — | 1 | 8.30 |
| CHEMBL3115260 | — | — | 1 | 8.26 |
| CHEMBL603067 | — | — | 1 | 7.92 |
| CHEMBL3115264 | — | — | 1 | - |
| CHEMBL3115249 | — | — | 1 | - |
| CHEMBL3115250 | — | — | 1 | - |
| CHEMBL3115428 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3115255 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3115256 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3115258 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL601202 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3115265 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3115426 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3115261 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3115429 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3115266 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3115254 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3115257 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3115253 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3115427 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3115259 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3115263 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3115251 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3115248 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3115262 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3115431 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3115430 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3115252 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3115260 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL603067 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3115264 | — | IC50 | > | 20.0 | nM | - |
| CHEMBL3115249 | — | IC50 | > | 18.0 | nM | - |
| CHEMBL3115250 | — | IC50 | > | 18.0 | nM | - |
| CHEMBL3115428 | — | IC50 | - | — | - |