Assay Detail
Functional
CHEMBL692144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HDJ2 farnesylation in PSN-1 cells over 7 hr assay in the presence of 50% human serum.
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PSN-1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.42 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516874 | — | — | 1 | 9.42 |
| CHEMBL310586 | — | — | 1 | 9.24 |
| CHEMBL311561 | — | — | 1 | 9.00 |
| CHEMBL526466 | — | — | 1 | 8.52 |
| CHEMBL526521 | — | — | 1 | 8.36 |
| CHEMBL80702 | — | — | 2 | 8.22 |
| CHEMBL525368 | — | — | 1 | 8.00 |
| CHEMBL53821 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516874 | — | EC50 | = | 0.38 | nM | 9.42 |
| CHEMBL310586 | — | EC50 | = | 0.58 | nM | 9.24 |
| CHEMBL311561 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL526466 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL526521 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL80702 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL80702 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL525368 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL53821 | — | EC50 | = | 130.0 | nM | 6.89 |