Assay Detail
Binding
CHEMBL1039874
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 PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay
39
Total Activities
34
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 | 39 | 7.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310570 | — | — | 1 | 9.00 |
| CHEMBL572356 | — | — | 1 | 8.74 |
| CHEMBL572212 | — | — | 1 | 8.70 |
| CHEMBL311662 | — | — | 1 | 8.66 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.60 |
| CHEMBL569044 | — | — | 1 | 8.30 |
| CHEMBL567027 | — | — | 1 | 8.12 |
| CHEMBL583629 | — | — | 1 | 8.03 |
| CHEMBL566575 | — | — | 1 | 8.02 |
| CHEMBL572330 | — | — | 1 | 7.96 |
| CHEMBL569544 | — | — | 1 | 7.80 |
| CHEMBL566600 | — | — | 1 | 7.75 |
| CHEMBL577945 | — | — | 1 | 7.70 |
| CHEMBL576472 | — | — | 1 | 7.60 |
| CHEMBL572329 | — | — | 1 | 7.55 |
| CHEMBL567028 | — | — | 1 | 7.54 |
| CHEMBL569061 | — | — | 1 | 7.51 |
| CHEMBL566387 | — | — | 1 | 7.47 |
| CHEMBL584522 | — | — | 1 | 7.43 |
| CHEMBL584258 | — | — | 1 | 7.28 |
| CHEMBL572355 | — | — | 1 | 7.24 |
| CHEMBL565320 | — | — | 1 | 7.24 |
| CHEMBL572357 | — | — | 1 | 7.23 |
| CHEMBL569290 | — | — | 1 | 6.96 |
| CHEMBL567237 | — | — | 1 | 6.88 |
| CHEMBL569543 | — | — | 4 | 6.74 |
| CHEMBL569100 | — | — | 1 | 6.64 |
| CHEMBL583858 | — | — | 2 | 6.57 |
| CHEMBL583859 | — | — | 1 | 6.55 |
| CHEMBL566823 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310570 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL572356 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL572212 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL311662 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL569044 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL567027 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL583629 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL566575 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL572330 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL569544 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL566600 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL577945 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL576472 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL572329 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL567028 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL569061 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL566387 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL584522 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL584258 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL572355 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL565320 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL572357 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL569290 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL567237 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL569543 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL569100 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL583858 | — | EC50 | = | 272.0 | nM | 6.57 |
| CHEMBL583859 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL566823 | — | EC50 | = | 324.0 | nM | 6.49 |
| CHEMBL583625 | — | EC50 | = | 573.0 | nM | 6.24 |
| CHEMBL569543 | — | EC50 | = | 1018.0 | nM | 5.99 |
| CHEMBL569543 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL566818 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566391 | — | EC50 | > | 2500.0 | nM | - |
| CHEMBL568868 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566391 | — | EC50 | > | 2500.0 | nM | - |
| CHEMBL583858 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL569543 | — | EC50 | > | 5000.0 | nM | - |