Assay Detail
Binding
CHEMBL681668
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Inhibition of [1-3H]-GGPP incorporation into biotinylated K4B-Ras peptide by geranylgeranyl transferase in the presence of 5 mM ATP
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.04 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64183 | — | — | 1 | 9.80 |
| CHEMBL63106 | — | — | 1 | 9.49 |
| CHEMBL63107 | — | — | 1 | 9.49 |
| CHEMBL291580 | — | — | 1 | 9.17 |
| CHEMBL303326 | — | — | 1 | 9.08 |
| CHEMBL59963 | — | — | 1 | 8.32 |
| CHEMBL418513 | — | — | 1 | 8.06 |
| CHEMBL302429 | — | — | 1 | 7.75 |
| CHEMBL305138 | — | — | 1 | 7.70 |
| CHEMBL304703 | — | — | 1 | 7.32 |
| CHEMBL63270 | — | — | 1 | 7.13 |
| CHEMBL293924 | — | — | 1 | 7.12 |
| CHEMBL293623 | — | — | 1 | 7.10 |
| CHEMBL293015 | — | — | 1 | 6.92 |
| CHEMBL64168 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64183 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL63106 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL63107 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL291580 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL303326 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL59963 | — | IC50 | = | 4.82 | nM | 8.32 |
| CHEMBL418513 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL302429 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL305138 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL304703 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL63270 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL293924 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL293623 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL293015 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL64168 | — | IC50 | = | 789.0 | nM | 6.10 |