Assay Detail
Binding
CHEMBL680824
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Inhibition of farnesyltransferase
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110187 | — | — | 1 | 9.00 |
| CHEMBL351706 | BMS-214662 | 1.0 | 1 | 8.89 |
| CHEMBL165895 | — | — | 1 | 8.52 |
| CHEMBL163739 | — | — | 1 | 8.40 |
| CHEMBL351004 | — | — | 1 | 8.22 |
| CHEMBL349613 | — | — | 1 | 8.22 |
| CHEMBL350736 | — | — | 1 | 8.10 |
| CHEMBL165285 | — | — | 1 | 8.10 |
| CHEMBL166353 | — | — | 1 | 8.05 |
| CHEMBL423799 | — | — | 1 | 8.00 |
| CHEMBL348819 | — | — | 1 | 8.00 |
| CHEMBL164116 | — | — | 1 | 7.89 |
| CHEMBL351288 | — | — | 1 | 7.82 |
| CHEMBL350401 | — | — | 1 | 7.82 |
| CHEMBL350803 | — | — | 1 | 7.77 |
| CHEMBL164286 | — | — | 1 | 7.75 |
| CHEMBL2110188 | — | — | 1 | 7.72 |
| CHEMBL424023 | — | — | 1 | 7.72 |
| CHEMBL349443 | — | — | 1 | 7.66 |
| CHEMBL434879 | — | — | 1 | 7.64 |
| CHEMBL350545 | — | — | 1 | 7.64 |
| CHEMBL162968 | — | — | 1 | 7.58 |
| CHEMBL165519 | — | — | 1 | 7.58 |
| CHEMBL348850 | — | — | 1 | 7.33 |
| CHEMBL164798 | — | — | 1 | 7.27 |
| CHEMBL165454 | — | — | 1 | 7.27 |
| CHEMBL349203 | — | — | 1 | 7.26 |
| CHEMBL349598 | — | — | 1 | 7.21 |
| CHEMBL165072 | — | — | 1 | 7.11 |
| CHEMBL348772 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110187 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL351706 | BMS-214662 | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL165895 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL163739 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL351004 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL349613 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL350736 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL165285 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL166353 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL423799 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL348819 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL164116 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL351288 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL350401 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL350803 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL164286 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2110188 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL424023 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL349443 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL434879 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL350545 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL162968 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL165519 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL348850 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL164798 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL165454 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL349203 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL349598 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL165072 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL348772 | — | IC50 | = | 142.0 | nM | 6.85 |