Assay Detail
Functional
CHEMBL692145
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Inhibition of HDJ2 farnesylation in PSN-1 cells over 7 hr assay
9
Total Activities
9
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 | 8.72 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516874 | — | — | 1 | 9.92 |
| CHEMBL525369 | (1R,5R)-30-OXO-19-OXA-2,6,10,12-TETRAAZAHEXACYCLO[18.6.2.1^{2,5}.1^{14,18}.0^{8,12}.0^{23,27}]TRIACONTA-8,10,14(29),15,17,20(28),21,23(27)-OCTAENE-17-CARBONITRILE (STRUCTURAL MIX) | — | 1 | 9.74 |
| CHEMBL310586 | — | — | 1 | 9.17 |
| CHEMBL311561 | — | — | 1 | 8.80 |
| CHEMBL526466 | — | — | 1 | 8.52 |
| CHEMBL526521 | — | — | 1 | 8.52 |
| CHEMBL80702 | — | — | 1 | 8.37 |
| CHEMBL525368 | — | — | 1 | 8.16 |
| CHEMBL53821 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516874 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL525369 | (1R,5R)-30-OXO-19-OXA-2,6,10,12-TETRAAZAHEXACYCLO[18.6.2.1^{2,5}.1^{14,18}.0^{8,12}.0^{23,27}]TRIACONTA-8,10,14(29),15,17,20(28),21,23(27)-OCTAENE-17-CARBONITRILE (STRUCTURAL MIX) | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL310586 | — | EC50 | = | 0.67 | nM | 9.17 |
| CHEMBL311561 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL526466 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL526521 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL80702 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL525368 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL53821 | — | EC50 | = | 48.0 | nM | 7.32 |