Assay Detail
Binding
CHEMBL4137372
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-1,25D3 from C-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli BL21 (DE3) after 16 hrs by radioligand binding assay
5
Total Activities
5
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
Identification of the Histidine Residue in Vitamin D Receptor That Covalently Binds to Electrophilic Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 9.09 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL846 | CALCITRIOL | 4.0 | 1 | 10.40 |
| CHEMBL4176277 | — | — | 1 | 8.96 |
| CHEMBL4176693 | — | — | 1 | 8.74 |
| CHEMBL4166076 | — | — | 1 | 8.72 |
| CHEMBL4161578 | — | — | 1 | 8.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL846 | CALCITRIOL | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL4176277 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4176693 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4166076 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4161578 | — | IC50 | = | 2.3 | nM | 8.64 |