Assay Detail
Binding
CHEMBL3369319
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Allosteric inhibition of human recombinant FPPS using GPP and [3H]IPP as substrate incubated with enzyme for 10 mins prior to substrate addition by liquid scintillation counting analysis
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 |
Publication
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.80 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | 8.52 |
| CHEMBL923 | RISEDRONIC ACID | 4.0 | 1 | 8.22 |
| CHEMBL3087936 | — | — | 1 | 7.85 |
| CHEMBL2088339 | — | — | 1 | 7.75 |
| CHEMBL2347862 | — | — | 1 | 7.66 |
| CHEMBL98110 | — | — | 1 | 7.48 |
| CHEMBL1231307 | — | — | 1 | 6.04 |
| CHEMBL3299149 | — | — | 1 | 5.92 |
| CHEMBL3299051 | — | — | 1 | 5.48 |
| CHEMBL3299047 | — | — | 1 | 5.35 |
| CHEMBL3299049 | — | — | 1 | 4.58 |
| CHEMBL3299048 | — | — | 1 | - |
| CHEMBL3299050 | — | — | 1 | - |
| CHEMBL261311 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL923 | RISEDRONIC ACID | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3087936 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2088339 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2347862 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL98110 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1231307 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3299149 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3299051 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3299047 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3299049 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3299048 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3299050 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL261311 | — | IC50 | > | 800000.0 | nM | - |