Assay Detail
Functional
CHEMBL692129
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Transcriptional repression in HepG2 cells expressing human glucocorticoid receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 7.23 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7781 | — | — | 1 | 8.30 |
| CHEMBL273658 | — | — | 1 | 8.30 |
| CHEMBL267940 | — | — | 1 | 7.92 |
| CHEMBL266282 | AL-43 | — | 1 | 7.89 |
| CHEMBL8140 | — | — | 1 | 7.85 |
| CHEMBL267231 | — | — | 1 | 7.75 |
| CHEMBL8394 | — | — | 1 | 7.75 |
| CHEMBL440454 | — | — | 1 | 7.72 |
| CHEMBL268239 | — | — | 1 | 7.72 |
| CHEMBL8007 | — | — | 1 | 7.35 |
| CHEMBL8637 | — | — | 1 | 7.28 |
| CHEMBL7671 | — | — | 1 | 7.23 |
| CHEMBL7817 | — | — | 1 | 7.23 |
| CHEMBL8209 | — | — | 1 | 7.22 |
| CHEMBL7655 | — | — | 1 | 7.09 |
| CHEMBL8027 | — | — | 1 | 7.09 |
| CHEMBL7988 | — | — | 1 | 7.09 |
| CHEMBL7987 | — | — | 1 | 7.03 |
| CHEMBL7843 | — | — | 1 | 7.00 |
| CHEMBL274208 | — | — | 1 | 6.92 |
| CHEMBL8055 | — | — | 1 | 6.89 |
| CHEMBL8329 | — | — | 1 | 6.85 |
| CHEMBL415309 | — | — | 1 | 6.81 |
| CHEMBL266488 | — | — | 1 | 6.80 |
| CHEMBL266709 | — | — | 1 | 6.60 |
| CHEMBL8360 | — | — | 1 | 6.57 |
| CHEMBL267670 | — | — | 1 | 6.52 |
| CHEMBL8639 | — | — | 1 | 6.46 |
| CHEMBL8340 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7781 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL273658 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL267940 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL266282 | AL-43 | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL8140 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL267231 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL8394 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL440454 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL268239 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL8007 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL8637 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL7671 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL7817 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL8209 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL7655 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL8027 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL7988 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL7987 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL7843 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL274208 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL8055 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL8329 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL415309 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL266488 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL266709 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL8360 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL267670 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL8639 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL8340 | — | EC50 | = | 467.0 | nM | 6.33 |