Assay Detail
Functional
CHEMBL751320
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of anchorage independent growth of H-ras transformed NIH3T3 cells in Soft Agar
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | NIH3T3 |
| Confidence | 1 — Organism |
| Curated By | Expert |
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 |
|---|---|---|---|
| EC50 | 16 | 7.09 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331640 | — | — | 1 | 8.00 |
| CHEMBL118669 | — | — | 1 | 8.00 |
| CHEMBL118181 | — | — | 1 | 7.89 |
| CHEMBL330945 | — | — | 1 | 7.82 |
| CHEMBL351706 | BMS-214662 | 1.0 | 1 | 7.60 |
| CHEMBL421235 | — | — | 1 | 7.52 |
| CHEMBL330815 | — | — | 1 | 7.40 |
| CHEMBL118616 | — | — | 1 | 7.30 |
| CHEMBL120683 | — | — | 1 | 7.00 |
| CHEMBL120071 | — | — | 1 | 6.57 |
| CHEMBL119771 | — | — | 1 | 6.54 |
| CHEMBL333251 | — | — | 1 | 6.52 |
| CHEMBL334073 | — | — | 1 | 6.40 |
| CHEMBL333589 | — | — | 1 | 6.34 |
| CHEMBL118526 | — | — | 1 | 6.28 |
| CHEMBL333288 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331640 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL118669 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL118181 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL330945 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL351706 | BMS-214662 | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL421235 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL330815 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL118616 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL120683 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL120071 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL119771 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL333251 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL334073 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL333589 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL118526 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL333288 | — | EC50 | = | 600.0 | nM | 6.22 |