Assay Detail
Binding
CHEMBL686002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of the human Geranylgeranyl transferase-catalyzed incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminal of human K-Ras.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.15 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL127617 | — | — | 1 | 6.96 |
| CHEMBL124081 | — | — | 1 | 6.91 |
| CHEMBL340122 | — | — | 1 | 6.82 |
| CHEMBL126270 | — | — | 1 | 6.82 |
| CHEMBL338148 | — | — | 1 | 6.80 |
| CHEMBL127155 | — | — | 1 | 6.66 |
| CHEMBL124339 | — | — | 1 | 6.51 |
| CHEMBL338853 | — | — | 1 | 6.31 |
| CHEMBL125907 | — | — | 1 | 6.27 |
| CHEMBL124470 | — | — | 1 | 6.07 |
| CHEMBL421641 | — | — | 1 | 5.89 |
| CHEMBL124525 | — | — | 1 | 5.80 |
| CHEMBL332230 | — | — | 1 | 5.75 |
| CHEMBL123792 | — | — | 1 | 5.75 |
| CHEMBL127296 | — | — | 1 | 5.46 |
| CHEMBL331224 | — | — | 1 | 5.05 |
| CHEMBL123687 | — | — | 1 | 4.80 |
| CHEMBL339230 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL127617 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL124081 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL340122 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL126270 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL338148 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL127155 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL124339 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL338853 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL125907 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL124470 | — | IC50 | = | 845.0 | nM | 6.07 |
| CHEMBL421641 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL124525 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL332230 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL123792 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL127296 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL331224 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL123687 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL339230 | — | IC50 | > | 10000.0 | nM | - |