Assay Detail
Binding
CHEMBL681886
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Inhibitor of Farnesyl protein transferase (FTPase) required to reduce radiolabel [1-3H] incorporation by 50%
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.10 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64183 | — | — | 1 | 9.44 |
| CHEMBL293623 | — | — | 1 | 8.82 |
| CHEMBL63107 | — | — | 1 | 8.80 |
| CHEMBL59963 | — | — | 1 | 8.60 |
| CHEMBL303326 | — | — | 1 | 8.51 |
| CHEMBL418513 | — | — | 1 | 8.30 |
| CHEMBL63106 | — | — | 1 | 8.21 |
| CHEMBL304449 | — | — | 1 | 8.19 |
| CHEMBL291580 | — | — | 1 | 8.17 |
| CHEMBL63270 | — | — | 1 | 7.87 |
| CHEMBL305138 | — | — | 1 | 7.81 |
| CHEMBL304703 | — | — | 1 | 7.75 |
| CHEMBL64168 | — | — | 1 | 7.72 |
| CHEMBL293924 | — | — | 1 | 7.47 |
| CHEMBL302429 | — | — | 1 | 7.00 |
| CHEMBL293015 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64183 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL293623 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL63107 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL59963 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL303326 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL418513 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL63106 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL304449 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL291580 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL63270 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL305138 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL304703 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL64168 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL293924 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL302429 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL293015 | — | IC50 | = | 102.0 | nM | 6.99 |