Assay Detail
Binding
CHEMBL685969
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Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Rat1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.62 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23155 | — | — | 1 | 9.72 |
| CHEMBL23650 | — | — | 1 | 9.32 |
| CHEMBL283369 | — | — | 1 | 9.09 |
| CHEMBL23248 | — | — | 1 | 8.96 |
| CHEMBL23460 | — | — | 1 | 8.92 |
| CHEMBL23411 | — | — | 1 | 8.70 |
| CHEMBL277413 | — | — | 1 | 7.92 |
| CHEMBL23939 | — | — | 1 | 7.54 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 7.02 |
| CHEMBL23163 | — | — | 1 | 6.80 |
| CHEMBL23218 | — | — | 1 | 6.71 |
| CHEMBL23239 | — | — | 1 | 6.60 |
| CHEMBL283542 | — | — | 1 | 6.36 |
| CHEMBL23490 | — | — | 1 | 6.22 |
| CHEMBL283380 | — | — | 1 | 6.18 |
| CHEMBL23135 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23155 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL23650 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL283369 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL23248 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL23460 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL23411 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL277413 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL23939 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL23163 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL23218 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL23239 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL283542 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL23490 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL283380 | — | IC50 | = | 662.0 | nM | 6.18 |
| CHEMBL23135 | — | IC50 | = | 1600.0 | nM | 5.80 |