Assay Detail
Functional
CHEMBL687558
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of geranylgeranylation of the C-terminal CAAX sequence of Rap 1a in PSN-1 cells
3
Total Activities
3
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 |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 7.40 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64183 | — | — | 1 | 7.75 |
| CHEMBL59963 | — | — | 1 | 7.30 |
| CHEMBL63107 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64183 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL59963 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL63107 | — | EC50 | = | 71.0 | nM | 7.15 |