Assay Detail
Functional
CHEMBL943880
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Antagonist activity at human FXR expressed in monkey CV1 cells after 24 hrs by ecdysone receptor response element-driven luciferase reporter assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.75 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251695 | — | — | 1 | 5.62 |
| CHEMBL402063 | E-GUGGULSTERONE | — | 1 | 5.39 |
| CHEMBL251696 | — | — | 1 | 4.62 |
| CHEMBL250263 | — | — | 1 | 4.50 |
| CHEMBL269105 | — | — | 1 | 4.22 |
| CHEMBL399743 | — | — | 1 | 4.12 |
| CHEMBL438521 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251695 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL402063 | E-GUGGULSTERONE | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL251696 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL250263 | — | IC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL269105 | — | IC50 | = | 60400.0 | nM | 4.22 |
| CHEMBL399743 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL438521 | — | IC50 | > | 100000.0 | nM | - |