Assay Detail
Binding
CHEMBL2061569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR after overnight incubation by scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 9.88 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2059272 | — | — | 1 | 10.70 |
| CHEMBL2059269 | — | — | 1 | 10.40 |
| CHEMBL2059271 | — | — | 1 | 10.22 |
| CHEMBL846 | CALCITRIOL | 4.0 | 1 | 10.00 |
| CHEMBL605525 | DP001 | 2.0 | 1 | 10.00 |
| CHEMBL2059268 | — | — | 1 | 10.00 |
| CHEMBL2059267 | — | — | 1 | 9.70 |
| CHEMBL2059270 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2059272 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL2059269 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL2059271 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL846 | CALCITRIOL | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL605525 | DP001 | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2059268 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2059267 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2059270 | — | Ki | = | 10.0 | nM | 8.00 |