Assay Detail
Binding
CHEMBL4382912
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His6-tagged GGPPS Y246D mutant expressed in Escherichia coli BL21(DE3) using [14C]-IPP and FPP as substrates after 10 mins by scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Geranylgeranyl pyrophosphate synthase (CHEMBL4769) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.09 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4471037 | — | — | 1 | 7.43 |
| CHEMBL4455060 | — | — | 1 | 7.41 |
| CHEMBL4465832 | — | — | 1 | 7.30 |
| CHEMBL4577077 | — | — | 1 | 7.12 |
| CHEMBL4564934 | — | — | 1 | 7.04 |
| CHEMBL258994 | DIGERANYL BISPHOSPHONATE | — | 1 | 6.23 |
| CHEMBL434024 | — | — | 1 | - |
| CHEMBL2347858 | — | — | 1 | - |
| CHEMBL2347859 | — | — | 1 | - |
| CHEMBL2347861 | — | — | 1 | - |
| CHEMBL4472025 | — | — | 1 | - |
| CHEMBL4538679 | — | — | 1 | - |
| CHEMBL4438154 | — | — | 1 | - |
| CHEMBL3087934 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4471037 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4455060 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4465832 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4577077 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4564934 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL258994 | DIGERANYL BISPHOSPHONATE | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL434024 | — | IC50 | - | — | - | |
| CHEMBL2347858 | — | IC50 | - | — | - | |
| CHEMBL2347859 | — | IC50 | - | — | - | |
| CHEMBL2347861 | — | IC50 | - | — | - | |
| CHEMBL4472025 | — | IC50 | - | — | - | |
| CHEMBL4538679 | — | IC50 | - | — | - | |
| CHEMBL4438154 | — | IC50 | - | — | - | |
| CHEMBL3087934 | — | IC50 | - | — | - |