Assay Detail
Binding
CHEMBL681128
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Inhibition of Farnesyltransferase in H-ras-transformed Rat cells by radiotracer assay (CRAFTI)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Protein farnesyltransferase (CHEMBL2095197) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.56 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312459 | — | — | 1 | 8.19 |
| CHEMBL524909 | — | — | 1 | 7.89 |
| CHEMBL310943 | — | — | 1 | 7.47 |
| CHEMBL312034 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312459 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL524909 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL310943 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL312034 | — | IC50 | = | 210.0 | nM | 6.68 |