Assay Detail
Functional
CHEMBL1052501
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Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay
27
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 9.06 | 10.40 |
| Emax | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1676 | FLUTICASONE FUROATE | 4.0 | 2 | 10.40 |
| CHEMBL551816 | — | — | 3 | 10.10 |
| CHEMBL550730 | — | — | 3 | 9.90 |
| CHEMBL564160 | — | — | 1 | 9.70 |
| CHEMBL563812 | — | — | 1 | 9.60 |
| CHEMBL560797 | — | — | 1 | 9.60 |
| CHEMBL556231 | — | — | 1 | 9.50 |
| CHEMBL550933 | — | — | 1 | 9.50 |
| CHEMBL559115 | — | — | 1 | 9.50 |
| CHEMBL559942 | — | — | 1 | 9.40 |
| CHEMBL561475 | — | — | 1 | 9.40 |
| CHEMBL550258 | — | — | 1 | 9.30 |
| CHEMBL561276 | — | — | 1 | 9.10 |
| CHEMBL563595 | — | — | 1 | 9.10 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 9.00 |
| CHEMBL394168 | — | — | 1 | 8.80 |
| CHEMBL559547 | — | — | 1 | 8.60 |
| CHEMBL558716 | — | — | 1 | 8.50 |
| CHEMBL559742 | — | — | 1 | 8.30 |
| CHEMBL559546 | — | — | 1 | 8.10 |
| CHEMBL562337 | — | — | 1 | 7.60 |
| CHEMBL564332 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1676 | FLUTICASONE FUROATE | IC50 | = | 0.03981 | nM | 10.40 |
| CHEMBL551816 | — | IC50 | = | 0.07943 | nM | 10.10 |
| CHEMBL551816 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL550730 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL564160 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL550730 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL563812 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL560797 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL556231 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL550933 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL559115 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL561475 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL559942 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL550258 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL561276 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL563595 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL394168 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL559547 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL558716 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL559742 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL559546 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL551816 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL562337 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL550730 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL564332 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1676 | FLUTICASONE FUROATE | Emax | = | 102.0 | % | - |