Assay Detail
Binding
CHEMBL681409
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In vitro inhibition of farnesyltransferase purified from bovine brain using scintillation proximity assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.55 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL123019 | — | — | 1 | 10.00 |
| CHEMBL333575 | — | — | 1 | 10.00 |
| CHEMBL108161 | — | — | 1 | 10.00 |
| CHEMBL122678 | — | — | 1 | 9.70 |
| CHEMBL274122 | — | — | 1 | 9.40 |
| CHEMBL124229 | — | — | 1 | 9.40 |
| CHEMBL421269 | — | — | 1 | 9.40 |
| CHEMBL121921 | — | — | 1 | 9.40 |
| CHEMBL123339 | — | — | 1 | 9.40 |
| CHEMBL331521 | — | — | 1 | 9.30 |
| CHEMBL122882 | — | — | 1 | 9.10 |
| CHEMBL122086 | — | — | 1 | 9.00 |
| CHEMBL332149 | — | — | 1 | 8.85 |
| CHEMBL330822 | — | — | 1 | 8.85 |
| CHEMBL121863 | — | — | 1 | 8.70 |
| CHEMBL122362 | — | — | 1 | 8.52 |
| CHEMBL420336 | — | — | 1 | 8.15 |
| CHEMBL421253 | — | — | 1 | 8.15 |
| CHEMBL432412 | — | — | 1 | 7.96 |
| CHEMBL414819 | — | — | 1 | 7.92 |
| CHEMBL122794 | — | — | 1 | 7.80 |
| CHEMBL333525 | — | — | 1 | 7.54 |
| CHEMBL121759 | — | — | 1 | 7.41 |
| CHEMBL331766 | — | — | 1 | 7.28 |
| CHEMBL124403 | — | — | 1 | 7.02 |
| CHEMBL122829 | — | — | 1 | 6.43 |
| CHEMBL122103 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL123019 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL333575 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL108161 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL122678 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL274122 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL124229 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL421269 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL121921 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL123339 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL331521 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL122882 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL122086 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL332149 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL330822 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL121863 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL122362 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL420336 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL421253 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL432412 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL414819 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL122794 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL333525 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL121759 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL331766 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL124403 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL122829 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL122103 | — | IC50 | = | 510.0 | nM | 6.29 |