Assay Detail
Binding
CHEMBL681749
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Binding affinity towards glucocorticoid receptor (GR) by displacing [3H]dexamethasone
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.78 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL266282 | AL-43 | — | 3 | 8.85 |
| CHEMBL337112 | — | — | 1 | 8.68 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.62 |
| CHEMBL138098 | — | — | 1 | 8.57 |
| CHEMBL140336 | — | — | 1 | 8.43 |
| CHEMBL97206 | — | — | 1 | 8.40 |
| CHEMBL336041 | — | — | 1 | 8.30 |
| CHEMBL343135 | — | — | 1 | 8.09 |
| CHEMBL141915 | — | — | 1 | 8.09 |
| CHEMBL137890 | — | — | 1 | 8.05 |
| CHEMBL141282 | — | — | 1 | 8.05 |
| CHEMBL137982 | — | — | 1 | 8.02 |
| CHEMBL141524 | — | — | 1 | 8.00 |
| CHEMBL141344 | — | — | 1 | 7.85 |
| CHEMBL138197 | — | — | 1 | 7.75 |
| CHEMBL138003 | — | — | 1 | 7.60 |
| CHEMBL141836 | — | — | 1 | 7.30 |
| CHEMBL141426 | — | — | 1 | 7.21 |
| CHEMBL138957 | — | — | 1 | 6.97 |
| CHEMBL140553 | — | — | 1 | 6.68 |
| CHEMBL141361 | — | — | 1 | 6.29 |
| CHEMBL138753 | — | — | 1 | 5.50 |
| CHEMBL138737 | — | — | 1 | - |
| CHEMBL342819 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL266282 | AL-43 | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL337112 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL131 | PREDNISOLONE | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL266282 | AL-43 | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL138098 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL140336 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL97206 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL336041 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL343135 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL141915 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL137890 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL141282 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL137982 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL141524 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL141344 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL138197 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL138003 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL141836 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL141426 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL138957 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL266282 | AL-43 | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL140553 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL141361 | — | Ki | = | 511.0 | nM | 6.29 |
| CHEMBL138753 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL138737 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL342819 | — | Ki | > | 5000.0 | nM | - |