Assay Detail
Binding
CHEMBL3370901
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in human whole blood assessed as inhibition of LPS-induced TNF production incubated for 20 hrs prior to LPS challenge measured after 5 hrs by ELISA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.49 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.16 |
| CHEMBL3315061 | — | — | 1 | 7.69 |
| CHEMBL3315062 | — | — | 1 | 7.67 |
| CHEMBL3315052 | — | — | 1 | 7.06 |
| CHEMBL3315069 | — | — | 1 | 6.70 |
| CHEMBL3315067 | — | — | 1 | 6.68 |
| CHEMBL3315065 | — | — | 1 | 6.68 |
| CHEMBL3315051 | — | — | 1 | 6.66 |
| CHEMBL3315068 | — | — | 1 | 6.56 |
| CHEMBL3315070 | — | — | 1 | 6.45 |
| CHEMBL3315049 | — | — | 1 | 6.42 |
| CHEMBL3315053 | — | — | 1 | 6.41 |
| CHEMBL3315054 | — | — | 1 | 6.38 |
| CHEMBL1911270 | — | — | 1 | 6.08 |
| CHEMBL3315057 | — | — | 1 | 5.99 |
| CHEMBL3315050 | — | — | 1 | 5.72 |
| CHEMBL3315058 | — | — | 1 | 5.67 |
| CHEMBL3315059 | — | — | 1 | 5.62 |
| CHEMBL3315055 | — | — | 1 | 5.62 |
| CHEMBL3315063 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3315061 | — | EC50 | = | 20.3 | nM | 7.69 |
| CHEMBL3315062 | — | EC50 | = | 21.5 | nM | 7.67 |
| CHEMBL3315052 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3315069 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3315067 | — | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL3315065 | — | EC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3315051 | — | EC50 | = | 218.0 | nM | 6.66 |
| CHEMBL3315068 | — | EC50 | = | 277.0 | nM | 6.56 |
| CHEMBL3315070 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3315049 | — | EC50 | = | 379.0 | nM | 6.42 |
| CHEMBL3315053 | — | EC50 | = | 389.0 | nM | 6.41 |
| CHEMBL3315054 | — | EC50 | = | 418.0 | nM | 6.38 |
| CHEMBL1911270 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3315057 | — | EC50 | = | 1035.0 | nM | 5.99 |
| CHEMBL3315050 | — | EC50 | = | 1892.0 | nM | 5.72 |
| CHEMBL3315058 | — | EC50 | = | 2143.0 | nM | 5.67 |
| CHEMBL3315059 | — | EC50 | = | 2378.0 | nM | 5.62 |
| CHEMBL3315055 | — | EC50 | = | 2378.0 | nM | 5.62 |
| CHEMBL3315063 | — | EC50 | = | 3054.0 | nM | 5.51 |