Assay Detail
Binding
CHEMBL3091236
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Inhibition of human recombinant FPPS using GPP/[3H]IPP as substrate incubated for 10 mins prior to substrate addition measured after 8 mins by scintillation counting analysis
12
Total Activities
12
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
Thienopyrimidine bisphosphonate (ThPBP) inhibitors of the human farnesyl pyrophosphate synthase: optimization and characterization of the mode of inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.49 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL923 | RISEDRONIC ACID | 4.0 | 1 | 8.28 |
| CHEMBL3087938 | — | — | 1 | 7.96 |
| CHEMBL3087936 | — | — | 1 | 7.85 |
| CHEMBL3087933 | — | — | 1 | 7.82 |
| CHEMBL2088339 | — | — | 1 | 7.75 |
| CHEMBL3087934 | — | — | 1 | 7.68 |
| CHEMBL2347862 | — | — | 1 | 7.66 |
| CHEMBL3087937 | — | — | 1 | 7.41 |
| CHEMBL2347863 | — | — | 1 | 7.20 |
| CHEMBL3087935 | — | — | 1 | 6.70 |
| CHEMBL1231307 | — | — | 1 | 6.04 |
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL923 | RISEDRONIC ACID | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3087938 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3087936 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3087933 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2088339 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3087934 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2347862 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3087937 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2347863 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3087935 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1231307 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | - | — | - |