Assay Detail
Binding
CHEMBL681298
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In vitro ability to displace radiolabeled FTI from farnesyltransferase in cultured Ha-ras transformed RAT1 cells
24
Total Activities
24
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 |
Target
Protein farnesyltransferase (CHEMBL2095197) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.07 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54212 | — | — | 1 | 8.15 |
| CHEMBL53069 | — | — | 1 | 7.89 |
| CHEMBL418268 | — | — | 1 | 7.82 |
| CHEMBL299568 | — | — | 1 | 7.77 |
| CHEMBL54043 | — | — | 1 | 7.77 |
| CHEMBL298895 | — | — | 1 | 7.64 |
| CHEMBL298392 | — | — | 1 | 7.53 |
| CHEMBL52975 | — | — | 1 | 7.43 |
| CHEMBL52921 | — | — | 1 | 7.37 |
| CHEMBL53183 | — | — | 1 | 7.26 |
| CHEMBL50857 | — | — | 1 | 7.19 |
| CHEMBL53811 | — | — | 1 | 7.17 |
| CHEMBL53037 | — | — | 1 | 7.00 |
| CHEMBL53862 | — | — | 1 | 6.74 |
| CHEMBL301491 | — | — | 1 | 6.71 |
| CHEMBL300966 | — | — | 1 | 6.62 |
| CHEMBL298337 | — | — | 1 | 6.61 |
| CHEMBL53154 | — | — | 1 | 6.59 |
| CHEMBL52610 | — | — | 1 | 6.51 |
| CHEMBL423303 | — | — | 1 | 6.39 |
| CHEMBL300206 | — | — | 1 | 6.39 |
| CHEMBL299621 | — | — | 1 | 6.24 |
| CHEMBL52859 | — | — | 1 | 5.88 |
| CHEMBL54969 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54212 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL53069 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL418268 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL299568 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL54043 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL298895 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL298392 | — | IC50 | = | 29.6 | nM | 7.53 |
| CHEMBL52975 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL52921 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL53183 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL50857 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL53811 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL53037 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL53862 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL301491 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL300966 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL298337 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL53154 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL52610 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL423303 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL300206 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL299621 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL52859 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL54969 | — | IC50 | > | 100.0 | nM | - |