Assay Detail
Binding
CHEMBL683490
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Inhibition of transfer of [3H]FPP to biotin K-ras peptide (KKSKTKCVIM) catalyzed by bovine GGTase-I
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Geranylgeranyl transferase type-1 subunit beta (CHEMBL4135) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 5.87 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43631 | — | — | 1 | 7.62 |
| CHEMBL41518 | — | — | 1 | 7.38 |
| CHEMBL38595 | — | — | 1 | 6.99 |
| CHEMBL37194 | — | — | 1 | 6.29 |
| CHEMBL41936 | — | — | 1 | 6.19 |
| CHEMBL38941 | — | — | 1 | 6.08 |
| CHEMBL289844 | — | — | 1 | 6.02 |
| CHEMBL38615 | — | — | 1 | 6.00 |
| CHEMBL288523 | — | — | 1 | 5.96 |
| CHEMBL41951 | — | — | 1 | 5.96 |
| CHEMBL39096 | — | — | 1 | 5.92 |
| CHEMBL41268 | — | — | 1 | 5.85 |
| CHEMBL38567 | — | — | 1 | 5.80 |
| CHEMBL38438 | — | — | 1 | 5.77 |
| CHEMBL434396 | — | — | 1 | 5.75 |
| CHEMBL39805 | — | — | 1 | 5.68 |
| CHEMBL288901 | — | — | 1 | 5.68 |
| CHEMBL290760 | — | — | 1 | 5.62 |
| CHEMBL38974 | — | — | 1 | 5.58 |
| CHEMBL288046 | — | — | 1 | 5.55 |
| CHEMBL418059 | — | — | 1 | 5.41 |
| CHEMBL43455 | — | — | 1 | 5.41 |
| CHEMBL39117 | — | — | 1 | 5.38 |
| CHEMBL43082 | — | — | 1 | 5.32 |
| CHEMBL41515 | — | — | 1 | 5.26 |
| CHEMBL41682 | — | — | 1 | 5.07 |
| CHEMBL38616 | — | — | 1 | 5.06 |
| CHEMBL41454 | — | — | 1 | - |
| CHEMBL41540 | — | — | 1 | - |
| CHEMBL432477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43631 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL41518 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL38595 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL37194 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL41936 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL38941 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL289844 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL38615 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL288523 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL41951 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL39096 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL41268 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL38567 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL38438 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL434396 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL39805 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL288901 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL290760 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL38974 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL288046 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL418059 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL43455 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL39117 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL43082 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL41515 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL41682 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL38616 | — | IC50 | = | 8620.0 | nM | 5.06 |
| CHEMBL41454 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL41540 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL432477 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL290161 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL288838 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL288449 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL287729 | — | IC50 | > | 10.0 | nM | - |