Assay Detail
Binding
CHEMBL5048366
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Inhibition of human FPPS expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins in presence compound relative to control
8
Total Activities
8
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
Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.43 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434024 | — | — | 1 | 8.40 |
| CHEMBL5088349 | — | — | 1 | 6.34 |
| CHEMBL2347859 | — | — | 1 | 6.26 |
| CHEMBL5082193 | — | — | 1 | 6.14 |
| CHEMBL4577077 | — | — | 1 | 5.89 |
| CHEMBL4465832 | — | — | 1 | 5.52 |
| CHEMBL5080121 | — | — | 1 | - |
| CHEMBL5089506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434024 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5088349 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2347859 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5082193 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4577077 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4465832 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5080121 | — | IC50 | - | — | - | |
| CHEMBL5089506 | — | IC50 | - | — | - |