Assay Detail
Binding
CHEMBL680084
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Inhibition of purified recombinant human farnesyltransferase (FT)
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.50 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL351706 | BMS-214662 | 1.0 | 1 | 8.87 |
| CHEMBL421235 | — | — | 1 | 8.81 |
| CHEMBL118669 | — | — | 1 | 8.75 |
| CHEMBL331640 | — | — | 1 | 8.75 |
| CHEMBL118616 | — | — | 1 | 8.54 |
| CHEMBL118181 | — | — | 1 | 8.52 |
| CHEMBL330945 | — | — | 1 | 8.22 |
| CHEMBL419048 | — | — | 1 | 8.10 |
| CHEMBL120683 | — | — | 1 | 8.06 |
| CHEMBL119771 | — | — | 1 | 7.97 |
| CHEMBL330815 | — | — | 1 | 7.80 |
| CHEMBL120499 | — | — | 1 | 7.77 |
| CHEMBL333589 | — | — | 1 | 7.75 |
| CHEMBL333251 | — | — | 1 | 7.66 |
| CHEMBL333423 | — | — | 1 | 7.63 |
| CHEMBL121797 | — | — | 1 | 7.62 |
| CHEMBL120071 | — | — | 1 | 7.52 |
| CHEMBL334073 | — | — | 1 | 7.35 |
| CHEMBL118526 | — | — | 1 | 7.26 |
| CHEMBL331654 | — | — | 1 | 7.26 |
| CHEMBL333288 | — | — | 1 | 7.22 |
| CHEMBL119993 | — | — | 1 | 7.07 |
| CHEMBL439601 | — | — | 1 | 7.00 |
| CHEMBL118496 | — | — | 1 | 6.56 |
| CHEMBL120548 | — | — | 1 | 6.42 |
| CHEMBL331391 | — | — | 1 | 6.36 |
| CHEMBL358680 | — | — | 1 | 6.34 |
| CHEMBL118896 | — | — | 1 | 5.96 |
| CHEMBL120595 | — | — | 1 | 5.90 |
| CHEMBL331101 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL351706 | BMS-214662 | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL421235 | — | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL118669 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL331640 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL118616 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL118181 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL330945 | — | IC50 | = | 5.95 | nM | 8.22 |
| CHEMBL419048 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL120683 | — | IC50 | = | 8.75 | nM | 8.06 |
| CHEMBL119771 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL330815 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL120499 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL333589 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL333251 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL333423 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL121797 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL120071 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL334073 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL118526 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL331654 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL333288 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL119993 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL439601 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL118496 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL120548 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL331391 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL358680 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL118896 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL120595 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL331101 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL121010 | — | IC50 | = | 228.0 | nM | - |