Assay Detail
Binding
CHEMBL5738950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Glucocorticoid Receptor Competitor Assay: The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen Glucocorticoid Receptor Competitor Assay Kit, Red (Life Technology, Catalog #A15898) according to the procedure in the kit. In brief, after compounds were diluted and transferred into assay plates, the fluormone GS red and GR full length protein were subsequently added into the assay plates, along with the positive and negative controls. The samples were mixed on a shaker for 1 minute and then the plates were incubated at room temperature for 2-4 hours with minimal light exposure. The plates were read with an Envision and the relative fluorescent signals were calculated. The data were plotted in GraphPad Prism and the EC50 values were calculated with non-linear regression curve fit of the data in GraphPad Prism.
66
Total Activities
22
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Phosphonate linkers and their use to facilitate cellular retention of compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.53 | 10.00 |
| kon | 22 | - | - |
| k_off | 22 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5927561 | — | — | 3 | 10.00 |
| CHEMBL5881550 | — | — | 3 | 9.85 |
| CHEMBL1201396 | FLUTICASONE | 3.0 | 3 | 9.82 |
| CHEMBL5758160 | — | — | 3 | 9.60 |
| CHEMBL5794824 | — | — | 3 | 9.49 |
| CHEMBL5833599 | — | — | 3 | 9.36 |
| CHEMBL5792934 | — | — | 3 | 9.35 |
| CHEMBL5901785 | — | — | 3 | 9.15 |
| CHEMBL1370 | BUDESONIDE | 4.0 | 3 | 9.05 |
| CHEMBL5812828 | — | — | 3 | 8.78 |
| CHEMBL5914440 | — | — | 3 | 8.70 |
| CHEMBL5999494 | — | — | 3 | 8.70 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 3 | 8.68 |
| CHEMBL6031431 | — | — | 3 | 8.62 |
| CHEMBL5855081 | — | — | 3 | 8.41 |
| CHEMBL5995932 | — | — | 3 | 8.39 |
| CHEMBL5885340 | — | — | 3 | 7.74 |
| CHEMBL5815679 | — | — | 3 | 7.62 |
| CHEMBL5758568 | — | — | 3 | 6.94 |
| CHEMBL5853572 | — | — | 3 | 6.80 |
| CHEMBL6053028 | — | — | 3 | 6.79 |
| CHEMBL6051178 | — | — | 3 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5927561 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5881550 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL1201396 | FLUTICASONE | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5758160 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5794824 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5833599 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5792934 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL5901785 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL1370 | BUDESONIDE | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5812828 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5999494 | — | IC50 | = | 1.99 | nM | 8.70 |
| CHEMBL5914440 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL6031431 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5855081 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5995932 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5885340 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL5815679 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL5758568 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5853572 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL6053028 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL6051178 | — | IC50 | = | 1225.0 | nM | 5.91 |
| CHEMBL5815679 | — | k_off | = | - | s-1 | - |
| CHEMBL5995932 | — | kon | = | - | — | - |
| CHEMBL5995932 | — | k_off | = | - | s-1 | - |
| CHEMBL5815679 | — | kon | = | - | — | - |
| CHEMBL5794824 | — | kon | = | - | — | - |
| CHEMBL384467 | DEXAMETHASONE | kon | = | - | — | - |
| CHEMBL384467 | DEXAMETHASONE | k_off | = | - | s-1 | - |
| CHEMBL1370 | BUDESONIDE | kon | = | - | — | - |
| CHEMBL1370 | BUDESONIDE | k_off | = | - | s-1 | - |
| CHEMBL1201396 | FLUTICASONE | kon | = | - | — | - |
| CHEMBL1201396 | FLUTICASONE | k_off | = | - | s-1 | - |
| CHEMBL5833599 | — | kon | = | - | — | - |
| CHEMBL5833599 | — | k_off | = | - | s-1 | - |
| CHEMBL5901785 | — | kon | = | - | — | - |
| CHEMBL5914440 | — | k_off | = | - | s-1 | - |
| CHEMBL6031431 | — | kon | = | - | — | - |
| CHEMBL5914440 | — | kon | = | - | — | - |
| CHEMBL6031431 | — | k_off | = | - | s-1 | - |
| CHEMBL5855081 | — | kon | = | - | — | - |
| CHEMBL5881550 | — | kon | = | - | — | - |
| CHEMBL5855081 | — | k_off | = | - | s-1 | - |
| CHEMBL5927561 | — | k_off | = | - | s-1 | - |
| CHEMBL5927561 | — | kon | = | - | — | - |
| CHEMBL5758568 | — | kon | = | - | — | - |
| CHEMBL5885340 | — | k_off | = | - | s-1 | - |
| CHEMBL5885340 | — | kon | = | - | — | - |
| CHEMBL5758568 | — | k_off | = | - | s-1 | - |
| CHEMBL5881550 | — | k_off | = | - | s-1 | - |