Assay Detail
Binding
CHEMBL681469
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Concentration required to displace 50% of a potent radiolabeled FTI from farnesyl transferase in cultured H-ras-transformed Rat1 cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Rat1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.36 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312137 | — | — | 1 | 9.28 |
| CHEMBL100661 | — | — | 1 | 8.96 |
| CHEMBL318438 | — | — | 1 | 8.57 |
| CHEMBL100798 | — | — | 1 | 8.48 |
| CHEMBL316502 | — | — | 1 | 8.24 |
| CHEMBL98361 | — | — | 1 | 8.21 |
| CHEMBL100566 | — | — | 1 | 8.02 |
| CHEMBL316726 | — | — | 1 | 7.92 |
| CHEMBL99381 | — | — | 1 | 7.85 |
| CHEMBL100579 | — | — | 1 | 7.68 |
| CHEMBL97925 | — | — | 1 | 7.57 |
| CHEMBL101561 | — | — | 1 | 7.52 |
| CHEMBL99205 | — | — | 1 | 7.52 |
| CHEMBL329732 | — | — | 1 | 7.44 |
| CHEMBL100415 | — | — | 1 | 7.38 |
| CHEMBL98974 | — | — | 1 | 7.31 |
| CHEMBL327500 | — | — | 1 | 7.28 |
| CHEMBL98553 | — | — | 1 | 7.19 |
| CHEMBL317520 | — | — | 1 | 7.17 |
| CHEMBL101467 | — | — | 1 | 7.16 |
| CHEMBL329067 | — | — | 1 | 7.13 |
| CHEMBL327946 | — | — | 1 | 6.96 |
| CHEMBL319737 | — | — | 1 | 6.92 |
| CHEMBL98147 | — | — | 1 | 6.82 |
| CHEMBL418982 | — | — | 1 | 6.82 |
| CHEMBL99371 | — | — | 1 | 6.70 |
| CHEMBL99435 | — | — | 1 | 6.62 |
| CHEMBL101788 | — | — | 1 | 6.52 |
| CHEMBL98711 | — | — | 1 | 6.51 |
| CHEMBL327278 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312137 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL100661 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL318438 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL100798 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL316502 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL98361 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL100566 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL316726 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL99381 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL100579 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL97925 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL101561 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL99205 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL329732 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL100415 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL98974 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL327500 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL98553 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL317520 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL101467 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL329067 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL327946 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL319737 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL98147 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL418982 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL99371 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL99435 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL101788 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL98711 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL327278 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL318943 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL317129 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL322007 | — | IC50 | = | 1100.0 | nM | 5.96 |