Assay Detail
Functional
CHEMBL686122
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity to reduce the human geranylgeranyl transferase type I (GGPTase-1)-catalyzed incorporation of 3H GGPP (100 nM) into K-Ras-derived peptide
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 6.27 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52610 | — | — | 1 | 7.54 |
| CHEMBL53154 | — | — | 1 | 7.30 |
| CHEMBL299568 | — | — | 1 | 7.18 |
| CHEMBL52921 | — | — | 1 | 7.14 |
| CHEMBL54212 | — | — | 1 | 7.11 |
| CHEMBL52859 | — | — | 1 | 6.83 |
| CHEMBL53811 | — | — | 1 | 6.82 |
| CHEMBL300206 | — | — | 1 | 6.60 |
| CHEMBL298895 | — | — | 1 | 6.50 |
| CHEMBL53862 | — | — | 1 | 6.46 |
| CHEMBL423303 | — | — | 1 | 6.33 |
| CHEMBL52975 | — | — | 1 | 6.17 |
| CHEMBL53037 | — | — | 1 | 6.05 |
| CHEMBL50857 | — | — | 1 | 5.96 |
| CHEMBL54969 | — | — | 1 | 5.91 |
| CHEMBL301491 | — | — | 1 | 5.68 |
| CHEMBL54043 | — | — | 1 | 5.50 |
| CHEMBL298337 | — | — | 1 | 5.32 |
| CHEMBL53183 | — | — | 1 | 5.17 |
| CHEMBL418268 | — | — | 1 | 5.17 |
| CHEMBL53069 | — | — | 1 | 4.89 |
| CHEMBL300966 | — | — | 1 | - |
| CHEMBL299621 | — | — | 1 | - |
| CHEMBL298392 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52610 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL53154 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL299568 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL52921 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL54212 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL52859 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL53811 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL300206 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL298895 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL53862 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL423303 | — | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL52975 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL53037 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL50857 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL54969 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL301491 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL54043 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL298337 | — | IC50 | = | 4820.0 | nM | 5.32 |
| CHEMBL53183 | — | IC50 | = | 6720.0 | nM | 5.17 |
| CHEMBL418268 | — | IC50 | = | 6760.0 | nM | 5.17 |
| CHEMBL53069 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL300966 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL299621 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL298392 | — | IC50 | > | 20000.0 | nM | - |