Assay Detail
Binding
CHEMBL2073174
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Inhibition of VDR-LBD expressed in human HEK293T cells co-expressing GAL4-DBD assessed as inhibition of 1,25-(OH)2D3-induced transcription after 24 hrs by FRET based GeneBLAzer assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.25 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070841 | — | — | 1 | 5.80 |
| CHEMBL2070844 | — | — | 1 | 5.58 |
| CHEMBL2070842 | — | — | 1 | 5.28 |
| CHEMBL2070858 | — | — | 1 | 5.26 |
| CHEMBL2070839 | — | — | 1 | 5.24 |
| CHEMBL2070859 | — | — | 1 | 5.22 |
| CHEMBL2070843 | — | — | 1 | 5.21 |
| CHEMBL1626334 | — | — | 1 | 5.17 |
| CHEMBL2070850 | — | — | 1 | 5.04 |
| CHEMBL1528294 | — | — | 1 | 4.97 |
| CHEMBL2070840 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070841 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2070844 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2070842 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2070858 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2070839 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2070859 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2070843 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1626334 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL2070850 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1528294 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL2070840 | — | IC50 | = | 11500.0 | nM | 4.94 |