Assay Detail
Functional
CHEMBL774952
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Inhibition of Rap1a protein geranylgeranylation in human PSN1 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | PSN1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.43 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316673 | — | — | 1 | 7.33 |
| CHEMBL450336 | — | — | 1 | 7.06 |
| CHEMBL439047 | — | — | 1 | 6.85 |
| CHEMBL318626 | — | — | 1 | 6.66 |
| CHEMBL99901 | — | — | 1 | 6.60 |
| CHEMBL294888 | — | — | 1 | 6.33 |
| CHEMBL2111612 | — | — | 1 | 6.14 |
| CHEMBL400694 | — | — | 1 | 5.50 |
| CHEMBL323302 | — | — | 1 | 5.40 |
| CHEMBL322435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316673 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL450336 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL439047 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL318626 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL99901 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL294888 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2111612 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL400694 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL323302 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL322435 | — | EC50 | > | 1000.0 | nM | - |