Assay Detail
Functional
CHEMBL680079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity to reduce the human farnesyltransferase catalyzed incorporation of [3H]FPP into recombinant Ras-CVIM
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.41 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52073 | — | — | 1 | 10.00 |
| CHEMBL299568 | — | — | 1 | 9.33 |
| CHEMBL423303 | — | — | 1 | 8.92 |
| CHEMBL298895 | — | — | 1 | 8.89 |
| CHEMBL52859 | — | — | 1 | 8.74 |
| CHEMBL52921 | — | — | 1 | 8.68 |
| CHEMBL53037 | — | — | 1 | 8.64 |
| CHEMBL300206 | — | — | 1 | 8.60 |
| CHEMBL298392 | — | — | 1 | 8.59 |
| CHEMBL53862 | — | — | 1 | 8.57 |
| CHEMBL53154 | — | — | 1 | 8.48 |
| CHEMBL53821 | — | — | 1 | 8.46 |
| CHEMBL52610 | — | — | 1 | 8.46 |
| CHEMBL53811 | — | — | 1 | 8.42 |
| CHEMBL52975 | — | — | 1 | 8.37 |
| CHEMBL54212 | — | — | 1 | 8.35 |
| CHEMBL301491 | — | — | 1 | 8.24 |
| CHEMBL50857 | — | — | 1 | 8.18 |
| CHEMBL54969 | — | — | 1 | 8.15 |
| CHEMBL53069 | — | — | 1 | 8.08 |
| CHEMBL298337 | — | — | 1 | 7.96 |
| CHEMBL418268 | — | — | 1 | 7.85 |
| CHEMBL53183 | — | — | 1 | 7.82 |
| CHEMBL54043 | — | — | 1 | 7.80 |
| CHEMBL300966 | — | — | 1 | 7.75 |
| CHEMBL299621 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52073 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL299568 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL423303 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL298895 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL52859 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL52921 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL53037 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL300206 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL298392 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL53862 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL53154 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL53821 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL52610 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL53811 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL52975 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL54212 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL301491 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL50857 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL54969 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL53069 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL298337 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL418268 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL53183 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL54043 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL300966 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL299621 | — | IC50 | = | 50.0 | nM | 7.30 |