Assay Detail
Binding
CHEMBL685884
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition against human Geranylgeranyl transferase type I catalyzed by incorporation of [3H]- GGPP (geranylgeranyl pyrophosphate) into biotinylated peptide corresponding to the c-terminus of human Ki-Ras
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.44 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281695 | — | — | 1 | 7.19 |
| CHEMBL30646 | — | — | 1 | 6.87 |
| CHEMBL31610 | — | — | 1 | 6.81 |
| CHEMBL418036 | — | — | 1 | 6.16 |
| CHEMBL30670 | — | — | 1 | 6.09 |
| CHEMBL283203 | — | — | 1 | 5.89 |
| CHEMBL439917 | — | — | 1 | 4.92 |
| CHEMBL30925 | — | — | 1 | 4.82 |
| CHEMBL31031 | — | — | 1 | 4.75 |
| CHEMBL30349 | — | — | 1 | 4.70 |
| CHEMBL30270 | — | — | 1 | 4.28 |
| CHEMBL30858 | — | — | 1 | 4.21 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 4.01 |
| CHEMBL31828 | — | — | 1 | - |
| CHEMBL29769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281695 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL30646 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL31610 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL418036 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL30670 | — | IC50 | = | 809.0 | nM | 6.09 |
| CHEMBL283203 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL439917 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL30925 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL31031 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL30349 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL30270 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL30858 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL31828 | — | IC50 | = | 199000.0 | nM | - |
| CHEMBL29769 | — | IC50 | = | 290000.0 | nM | - |