Assay Detail
Binding
CHEMBL1039876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay
35
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A549 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 7.11 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.96 |
| CHEMBL572330 | — | — | 1 | 7.96 |
| CHEMBL572329 | — | — | 1 | 7.75 |
| CHEMBL567027 | — | — | 1 | 7.72 |
| CHEMBL567028 | — | — | 1 | 7.52 |
| CHEMBL576472 | — | — | 1 | 7.51 |
| CHEMBL566600 | — | — | 1 | 7.51 |
| CHEMBL572212 | — | — | 1 | 7.48 |
| CHEMBL569044 | — | — | 1 | 7.43 |
| CHEMBL584258 | — | — | 1 | 7.39 |
| CHEMBL577945 | — | — | 1 | 7.36 |
| CHEMBL572355 | — | — | 1 | 7.32 |
| CHEMBL584522 | — | — | 1 | 7.31 |
| CHEMBL569544 | — | — | 1 | 7.21 |
| CHEMBL565320 | — | — | 1 | 7.10 |
| CHEMBL569290 | — | — | 1 | 7.04 |
| CHEMBL566575 | — | — | 1 | 7.00 |
| CHEMBL572357 | — | — | 1 | 6.98 |
| CHEMBL569100 | — | — | 1 | 6.92 |
| CHEMBL566387 | — | — | 1 | 6.89 |
| CHEMBL567237 | — | — | 1 | 6.88 |
| CHEMBL583858 | — | — | 2 | 6.61 |
| CHEMBL583859 | — | — | 1 | 6.40 |
| CHEMBL569543 | — | — | 4 | 6.04 |
| CHEMBL583625 | — | — | 1 | 6.03 |
| CHEMBL566823 | — | — | 1 | 5.56 |
| CHEMBL568868 | — | — | 1 | - |
| CHEMBL566818 | — | — | 1 | - |
| CHEMBL566391 | — | — | 2 | - |
| CHEMBL569061 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL572330 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL572329 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL567027 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL567028 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL566600 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL576472 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL572212 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL569044 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL584258 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL577945 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL572355 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL584522 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL569544 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL565320 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL569290 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL566575 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL572357 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL569100 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL566387 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL567237 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL583858 | — | EC50 | = | 243.0 | nM | 6.61 |
| CHEMBL583859 | — | EC50 | = | 398.0 | nM | 6.40 |
| CHEMBL569543 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL569543 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL583625 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL566823 | — | EC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL566818 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566391 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566391 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL568868 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL583858 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL569543 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL569543 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL569061 | — | EC50 | - | — | - |