Assay Detail
Functional
CHEMBL681407
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Inhibition of Farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 22 | 7.98 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23460 | — | — | 1 | 9.77 |
| CHEMBL23155 | — | — | 1 | 9.60 |
| CHEMBL23411 | — | — | 1 | 8.92 |
| CHEMBL277413 | — | — | 1 | 8.80 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 8.70 |
| CHEMBL23248 | — | — | 1 | 8.68 |
| CHEMBL23650 | — | — | 1 | 8.51 |
| CHEMBL23939 | — | — | 1 | 8.24 |
| CHEMBL283369 | — | — | 1 | 8.21 |
| CHEMBL280181 | — | — | 1 | 8.10 |
| CHEMBL23218 | — | — | 1 | 8.06 |
| CHEMBL283793 | — | — | 1 | 7.99 |
| CHEMBL23135 | — | — | 1 | 7.92 |
| CHEMBL23163 | — | — | 1 | 7.85 |
| CHEMBL23490 | — | — | 1 | 7.82 |
| CHEMBL23217 | — | — | 1 | 7.77 |
| CHEMBL23239 | — | — | 1 | 7.72 |
| CHEMBL283542 | — | — | 1 | 7.46 |
| CHEMBL23219 | — | — | 1 | 7.28 |
| CHEMBL22675 | — | — | 1 | 6.41 |
| CHEMBL283380 | — | — | 1 | 6.39 |
| CHEMBL282011 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23460 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL23155 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL23411 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL277413 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL23248 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL23650 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL23939 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL283369 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL280181 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL23218 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL283793 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL23135 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL23163 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL23490 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL23217 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL23239 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL283542 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL23219 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL22675 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL283380 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL282011 | — | IC50 | = | 3500.0 | nM | 5.46 |