Assay Detail
Binding
CHEMBL4042890
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Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production
12
Total Activities
12
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 new selective glucocorticoid receptor agonist leads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.22 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893393 | — | — | 1 | 9.80 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.60 |
| CHEMBL4082878 | — | — | 1 | 8.40 |
| CHEMBL4069357 | — | — | 1 | 8.30 |
| CHEMBL1257572 | — | — | 1 | 8.30 |
| CHEMBL3962413 | — | — | 1 | 8.20 |
| CHEMBL4090392 | — | — | 1 | 8.20 |
| CHEMBL4085241 | — | — | 1 | 8.20 |
| CHEMBL4092066 | — | — | 1 | 7.80 |
| CHEMBL4072079 | — | — | 1 | 7.70 |
| CHEMBL4098118 | — | — | 1 | 7.70 |
| CHEMBL4064352 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893393 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4082878 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4069357 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1257572 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3962413 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4090392 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4085241 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4092066 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4072079 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4098118 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4064352 | — | IC50 | = | 39.81 | nM | 7.40 |