Assay Detail
Binding
CHEMBL770239
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In vitro inhibition of [3H]GGPP incorporation into H-Ras-CVLL by Geranylgeranyl transferase type I
11
Total Activities
11
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
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.63 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26923 | — | — | 1 | 7.50 |
| CHEMBL26246 | — | — | 1 | 7.42 |
| CHEMBL28367 | — | — | 1 | 7.36 |
| CHEMBL27449 | — | — | 1 | 7.26 |
| CHEMBL281738 | — | — | 1 | 7.05 |
| CHEMBL27002 | — | — | 1 | 6.82 |
| CHEMBL26771 | — | — | 1 | 6.68 |
| CHEMBL26720 | — | — | 1 | 6.40 |
| CHEMBL282814 | — | — | 1 | 5.80 |
| CHEMBL282297 | — | — | 1 | 5.40 |
| CHEMBL285129 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26923 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL26246 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL28367 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL27449 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL281738 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL27002 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL26771 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL26720 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL282814 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL282297 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL285129 | — | IC50 | = | 6100.0 | nM | 5.21 |