Assay Detail
Functional
CHEMBL921913
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Antagonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.51 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409470 | — | — | 1 | 7.00 |
| CHEMBL263638 | — | — | 1 | 6.52 |
| CHEMBL429347 | — | — | 1 | 6.52 |
| CHEMBL261197 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409470 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL263638 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL429347 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL261197 | — | IC50 | = | 1000.0 | nM | 6.00 |