Assay Detail
ADMET
CHEMBL2025284
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Transactivation activity at glucocorticoid receptor in rat H4II-E cells assessed as induction of tyrosine aminotransferase
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Rattus norvegicus |
| Cell Type | H4II-E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.31 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2022651 | — | — | 1 | 8.49 |
| CHEMBL2022858 | — | — | 1 | 8.49 |
| CHEMBL2021945 | — | — | 1 | 8.35 |
| CHEMBL2023619 | — | — | 1 | 7.88 |
| CHEMBL2023620 | — | — | 1 | 7.84 |
| CHEMBL2023239 | — | — | 1 | 7.62 |
| CHEMBL2023614 | — | — | 1 | 7.61 |
| CHEMBL2022655 | — | — | 1 | 7.50 |
| CHEMBL2022656 | — | — | 1 | 7.47 |
| CHEMBL2023615 | — | — | 1 | 7.35 |
| CHEMBL2023243 | — | — | 1 | 7.28 |
| CHEMBL2023236 | — | — | 1 | 7.26 |
| CHEMBL2022859 | — | — | 1 | 7.24 |
| CHEMBL2023244 | — | — | 1 | 7.24 |
| CHEMBL2023618 | — | — | 1 | 7.18 |
| CHEMBL2023242 | — | — | 1 | 7.11 |
| CHEMBL2022653 | — | — | 1 | 7.11 |
| CHEMBL2023240 | — | — | 1 | 7.08 |
| CHEMBL2022660 | — | — | 1 | 7.08 |
| CHEMBL2023621 | — | — | 1 | 7.06 |
| CHEMBL2022862 | — | — | 1 | 6.95 |
| CHEMBL2022865 | — | — | 1 | 6.87 |
| CHEMBL2023241 | — | — | 1 | 6.76 |
| CHEMBL2022657 | — | — | 1 | 6.65 |
| CHEMBL2022866 | — | — | 1 | 6.59 |
| CHEMBL2022654 | — | — | 1 | 6.00 |
| CHEMBL2023233 | — | — | 1 | - |
| CHEMBL2022860 | — | — | 1 | - |
| CHEMBL2022652 | — | — | 1 | - |
| CHEMBL2023234 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2022651 | — | IC50 | = | 3.23 | nM | 8.49 |
| CHEMBL2022858 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2021945 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2023619 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL2023620 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL2023239 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL2023614 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL2022655 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL2022656 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL2023615 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL2023243 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL2023236 | — | IC50 | = | 54.7 | nM | 7.26 |
| CHEMBL2022859 | — | IC50 | = | 57.3 | nM | 7.24 |
| CHEMBL2023244 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2023618 | — | IC50 | = | 65.4 | nM | 7.18 |
| CHEMBL2022653 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2023242 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2023240 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2022660 | — | IC50 | = | 82.3 | nM | 7.08 |
| CHEMBL2023621 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL2022862 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL2022865 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2023241 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL2022657 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL2022866 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL2022654 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2023233 | — | IC50 | - | — | - | |
| CHEMBL2022860 | — | IC50 | - | — | - | |
| CHEMBL2022652 | — | IC50 | - | — | - | |
| CHEMBL2023234 | — | IC50 | - | — | - | |
| CHEMBL2023235 | — | IC50 | - | — | - | |
| CHEMBL2023237 | — | IC50 | - | — | - | |
| CHEMBL2023238 | — | IC50 | - | — | - |