Assay Detail
Binding
CHEMBL684165
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Inhibition of human Geranylgeranyl transferase type I incorporation of [3H]GGPP into biotinylated peptide corresponding to the C-terminus of human Ki-Ras.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.90 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL159171 | — | — | 1 | 8.77 |
| CHEMBL157295 | — | — | 1 | 8.68 |
| CHEMBL158586 | — | — | 1 | 8.62 |
| CHEMBL345474 | — | — | 1 | 7.37 |
| CHEMBL349329 | — | — | 1 | 7.34 |
| CHEMBL346589 | — | — | 1 | 7.26 |
| CHEMBL346771 | — | — | 1 | 7.01 |
| CHEMBL346084 | — | — | 1 | 7.00 |
| CHEMBL160223 | — | — | 1 | 6.97 |
| CHEMBL160204 | — | — | 1 | 6.91 |
| CHEMBL423062 | — | — | 1 | 6.67 |
| CHEMBL424338 | — | — | 1 | 6.62 |
| CHEMBL52073 | — | — | 1 | 6.52 |
| CHEMBL350680 | — | — | 1 | 6.38 |
| CHEMBL156586 | — | — | 1 | 6.35 |
| CHEMBL346700 | — | — | 1 | 6.30 |
| CHEMBL423241 | — | — | 1 | 6.27 |
| CHEMBL156225 | — | — | 1 | 5.98 |
| CHEMBL347018 | — | — | 1 | 5.56 |
| CHEMBL348336 | — | — | 1 | 5.42 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL159171 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL157295 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL158586 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL345474 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL349329 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL346589 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL346771 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL346084 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL160223 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL160204 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL423062 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL424338 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL52073 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL350680 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL156586 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL346700 | — | IC50 | = | 502.0 | nM | 6.30 |
| CHEMBL423241 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL156225 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL347018 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL348336 | — | IC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 98.0 | nM | - |