Assay Detail
Binding
CHEMBL682226
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In vitro FPT potency by measuring the ability to inhibit the transfer of [3H]farnesyl from farnesyl pyrophosphate to H-Ras-CLVS.
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.44 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430450 | — | — | 2 | 7.50 |
| CHEMBL311310 | — | — | 1 | 7.44 |
| CHEMBL311434 | — | — | 1 | 7.42 |
| CHEMBL81889 | — | — | 1 | 7.37 |
| CHEMBL313090 | — | — | 1 | 7.21 |
| CHEMBL423677 | — | — | 1 | 7.10 |
| CHEMBL85141 | — | — | 1 | 6.96 |
| CHEMBL87345 | — | — | 1 | 6.85 |
| CHEMBL421722 | — | — | 1 | 6.85 |
| CHEMBL315067 | — | — | 1 | 6.72 |
| CHEMBL289404 | — | — | 1 | 6.60 |
| CHEMBL309483 | — | — | 1 | 6.28 |
| CHEMBL82004 | — | — | 1 | 6.25 |
| CHEMBL85670 | — | — | 1 | 6.23 |
| CHEMBL315599 | — | — | 1 | 6.21 |
| CHEMBL82505 | — | — | 1 | 6.08 |
| CHEMBL313193 | — | — | 1 | 6.04 |
| CHEMBL86103 | — | — | 1 | 6.00 |
| CHEMBL85564 | — | — | 1 | 5.96 |
| CHEMBL85663 | — | — | 1 | 5.95 |
| CHEMBL316005 | — | — | 1 | 5.82 |
| CHEMBL85671 | — | — | 1 | 5.75 |
| CHEMBL85529 | — | — | 1 | 5.68 |
| CHEMBL84036 | — | — | 1 | 5.57 |
| CHEMBL84711 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430450 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL311310 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL311434 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL81889 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL313090 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL423677 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL85141 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL87345 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL421722 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL315067 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL289404 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL309483 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL82004 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL85670 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL315599 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL82505 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL313193 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL430450 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL86103 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL85564 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL85663 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL316005 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL85671 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL85529 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL84036 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL84711 | — | IC50 | = | 3400.0 | nM | 5.47 |