Assay Detail
Binding
CHEMBL679579
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FPT inhibitory activity was determined by the ability to inhibit the transfer of [3H]farnesyl from farnesyl pyrophosphate to H-ras-CLVS
45
Total Activities
44
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 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 7.15 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348647 | — | — | 1 | 8.77 |
| CHEMBL352022 | — | — | 1 | 8.22 |
| CHEMBL440732 | — | — | 1 | 8.22 |
| CHEMBL155363 | — | — | 1 | 8.09 |
| CHEMBL348395 | — | — | 1 | 7.92 |
| CHEMBL155232 | — | — | 1 | 7.89 |
| CHEMBL155434 | — | — | 1 | 7.82 |
| CHEMBL157570 | — | — | 1 | 7.82 |
| CHEMBL153911 | — | — | 1 | 7.75 |
| CHEMBL443816 | — | — | 1 | 7.70 |
| CHEMBL345575 | — | — | 1 | 7.54 |
| CHEMBL345846 | — | — | 1 | 7.52 |
| CHEMBL154138 | — | — | 1 | 7.50 |
| CHEMBL347625 | — | — | 1 | 7.46 |
| CHEMBL347003 | — | — | 1 | 7.42 |
| CHEMBL347798 | — | — | 1 | 7.42 |
| CHEMBL155381 | — | — | 1 | 7.38 |
| CHEMBL348576 | — | — | 1 | 7.37 |
| CHEMBL157908 | — | — | 1 | 7.37 |
| CHEMBL348110 | — | — | 1 | 7.24 |
| CHEMBL158245 | — | — | 1 | 7.21 |
| CHEMBL415739 | — | — | 1 | 7.13 |
| CHEMBL434857 | — | — | 1 | 7.09 |
| CHEMBL157803 | — | — | 1 | 7.08 |
| CHEMBL433885 | — | — | 1 | 7.07 |
| CHEMBL41934 | — | — | 1 | 7.05 |
| CHEMBL440365 | — | — | 1 | 7.00 |
| CHEMBL348370 | — | — | 1 | 6.98 |
| CHEMBL346039 | — | — | 1 | 6.94 |
| CHEMBL154417 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348647 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL352022 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL440732 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL155363 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL348395 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL155232 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL157570 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL155434 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL153911 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL443816 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL345575 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL345846 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL154138 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL347625 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL347003 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL347798 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL155381 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL157908 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL348576 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL348110 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL158245 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL415739 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL434857 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL157803 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL433885 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL41934 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL440365 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL348370 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL346039 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL154417 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL156431 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL156989 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL347031 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL156462 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL158324 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL348280 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL155766 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL346806 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL346484 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL338697 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL338697 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL154303 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL154710 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL1172 | DESLORATADINE | IC50 | > | 65000.0 | nM | - |
| CHEMBL358448 | — | IC50 | < | 110.0 | nM | - |