Assay Detail
Binding
CHEMBL1039878
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa |
| 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 | 26 | 6.53 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.35 |
| CHEMBL310570 | — | — | 1 | 7.44 |
| CHEMBL311662 | — | — | 1 | 7.24 |
| CHEMBL572330 | — | — | 1 | 6.60 |
| CHEMBL572329 | — | — | 1 | 6.57 |
| CHEMBL567028 | — | — | 1 | 6.42 |
| CHEMBL572212 | — | — | 1 | 6.33 |
| CHEMBL569290 | — | — | 1 | 6.24 |
| CHEMBL567027 | — | — | 1 | 6.16 |
| CHEMBL569100 | — | — | 1 | 6.12 |
| CHEMBL567237 | — | — | 1 | 6.06 |
| CHEMBL576472 | — | — | 1 | 6.04 |
| CHEMBL566575 | — | — | 1 | 5.95 |
| CHEMBL566387 | — | — | 1 | 5.95 |
| CHEMBL569044 | — | — | 1 | - |
| CHEMBL569544 | — | — | 1 | - |
| CHEMBL565320 | — | — | 1 | - |
| CHEMBL568868 | — | — | 1 | - |
| CHEMBL572357 | — | — | 1 | - |
| CHEMBL584522 | — | — | 1 | - |
| CHEMBL566600 | — | — | 1 | - |
| CHEMBL572355 | — | — | 1 | - |
| CHEMBL569061 | — | — | 1 | - |
| CHEMBL583859 | — | — | 1 | - |
| CHEMBL583625 | — | — | 1 | - |
| CHEMBL566823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL310570 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL311662 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL572330 | — | EC50 | = | 253.0 | nM | 6.60 |
| CHEMBL572329 | — | EC50 | = | 272.0 | nM | 6.57 |
| CHEMBL567028 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL572212 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL569290 | — | EC50 | = | 572.0 | nM | 6.24 |
| CHEMBL567027 | — | EC50 | = | 697.0 | nM | 6.16 |
| CHEMBL569100 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL567237 | — | EC50 | = | 876.0 | nM | 6.06 |
| CHEMBL576472 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL566575 | — | EC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL566387 | — | EC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL569044 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL569544 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL565320 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL568868 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL572357 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL584522 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566600 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL572355 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL569061 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL583859 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL583625 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566823 | — | EC50 | > | 10000.0 | nM | - |