Assay Detail
Binding
CHEMBL2073151
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of LG190178-induced VDR-LBD interaction to Alexa Fluor 647-labeled SRC2-3 after 3 hrs by fluorescence polarization assay
48
Total Activities
48
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
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 | 48 | 4.77 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1494735 | — | — | 1 | 5.70 |
| CHEMBL2070859 | — | — | 1 | 5.48 |
| CHEMBL2070858 | — | — | 1 | 5.41 |
| CHEMBL2070839 | — | — | 1 | 5.23 |
| CHEMBL2070843 | — | — | 1 | 5.16 |
| CHEMBL2070841 | — | — | 1 | 5.15 |
| CHEMBL2070842 | — | — | 1 | 5.09 |
| CHEMBL2070840 | — | — | 1 | 5.07 |
| CHEMBL2070845 | — | — | 1 | 5.02 |
| CHEMBL1528294 | — | — | 1 | 4.98 |
| CHEMBL2070857 | — | — | 1 | 4.98 |
| CHEMBL1626334 | — | — | 1 | 4.86 |
| CHEMBL2070856 | — | — | 1 | 4.86 |
| CHEMBL2070855 | — | — | 1 | 4.85 |
| CHEMBL2070847 | — | — | 1 | 4.85 |
| CHEMBL2070850 | — | — | 1 | 4.82 |
| CHEMBL2070848 | — | — | 1 | 4.76 |
| CHEMBL2070872 | — | — | 1 | 4.75 |
| CHEMBL2070853 | — | — | 1 | 4.69 |
| CHEMBL2070878 | — | — | 1 | 4.69 |
| CHEMBL142827 | — | — | 1 | 4.67 |
| CHEMBL2070852 | — | — | 1 | 4.66 |
| CHEMBL2070844 | — | — | 1 | 4.65 |
| CHEMBL2070876 | — | — | 1 | 4.61 |
| CHEMBL2070838 | — | — | 1 | 4.60 |
| CHEMBL2070851 | — | — | 1 | 4.60 |
| CHEMBL2070871 | — | — | 1 | 4.58 |
| CHEMBL2070846 | — | — | 1 | 4.56 |
| CHEMBL2070854 | — | — | 1 | 4.55 |
| CHEMBL2070865 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1494735 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2070859 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2070858 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL2070839 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2070843 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2070841 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2070842 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2070840 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2070845 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1528294 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL2070857 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL1626334 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL2070856 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL2070855 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL2070847 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL2070850 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL2070848 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL2070872 | — | IC50 | = | 17700.0 | nM | 4.75 |
| CHEMBL2070853 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL2070878 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL142827 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL2070852 | — | IC50 | = | 22100.0 | nM | 4.66 |
| CHEMBL2070844 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL2070876 | — | IC50 | = | 24300.0 | nM | 4.61 |
| CHEMBL2070838 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2070851 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL2070871 | — | IC50 | = | 26500.0 | nM | 4.58 |
| CHEMBL2070846 | — | IC50 | = | 27700.0 | nM | 4.56 |
| CHEMBL2070854 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2070865 | — | IC50 | = | 28500.0 | nM | 4.54 |
| CHEMBL2070849 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL2070870 | — | IC50 | = | 28500.0 | nM | 4.54 |
| CHEMBL2070867 | — | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL2070869 | — | IC50 | = | 29800.0 | nM | 4.53 |
| CHEMBL2070860 | — | IC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL2069323 | — | IC50 | = | 30300.0 | nM | 4.52 |
| CHEMBL2070862 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL2070861 | — | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL1327417 | — | IC50 | = | 37600.0 | nM | 4.42 |
| CHEMBL2070863 | — | IC50 | = | 43600.0 | nM | 4.36 |
| CHEMBL2070868 | — | IC50 | = | 58600.0 | nM | 4.23 |
| CHEMBL2070866 | — | IC50 | = | 104800.0 | nM | - |
| CHEMBL2070873 | — | IC50 | - | — | - | |
| CHEMBL2070874 | — | IC50 | - | — | - | |
| CHEMBL2070864 | — | IC50 | - | — | - | |
| CHEMBL2070875 | — | IC50 | - | — | - | |
| CHEMBL2070877 | — | IC50 | - | — | - | |
| CHEMBL2070879 | — | IC50 | - | — | - |