Assay Detail
Functional
CHEMBL950163
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | SW1353/MMTV5 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 65 | 7.73 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270575 | — | — | 1 | 9.22 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 8.92 |
| CHEMBL270668 | — | — | 1 | 8.92 |
| CHEMBL404183 | — | — | 1 | 8.80 |
| CHEMBL271221 | — | — | 1 | 8.72 |
| CHEMBL270667 | — | — | 1 | 8.54 |
| CHEMBL270143 | — | — | 1 | 8.51 |
| CHEMBL429913 | — | — | 1 | 8.47 |
| CHEMBL256161 | — | — | 1 | 8.33 |
| CHEMBL256894 | — | — | 1 | 8.31 |
| CHEMBL411852 | — | — | 1 | 8.29 |
| CHEMBL442803 | — | — | 1 | 8.28 |
| CHEMBL255369 | — | — | 1 | 8.24 |
| CHEMBL409835 | — | — | 1 | 8.24 |
| CHEMBL257462 | — | — | 1 | 8.24 |
| CHEMBL271220 | CORT 108297 | 1.0 | 1 | 8.17 |
| CHEMBL255950 | — | — | 1 | 8.16 |
| CHEMBL270838 | — | — | 1 | 8.15 |
| CHEMBL402893 | — | — | 1 | 8.11 |
| CHEMBL410037 | — | — | 1 | 8.10 |
| CHEMBL270568 | — | — | 1 | 8.06 |
| CHEMBL270879 | — | — | 1 | 8.05 |
| CHEMBL257203 | — | — | 1 | 8.00 |
| CHEMBL401864 | — | — | 1 | 7.96 |
| CHEMBL402351 | — | — | 1 | 7.96 |
| CHEMBL403179 | — | — | 1 | 7.96 |
| CHEMBL403761 | — | — | 1 | 7.85 |
| CHEMBL270588 | — | — | 1 | 7.85 |
| CHEMBL404160 | — | — | 1 | 7.80 |
| CHEMBL257204 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270575 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL270668 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL404183 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL271221 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL270667 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL270143 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL429913 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL256161 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL256894 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL411852 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL442803 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL409835 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL257462 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL255369 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL271220 | CORT 108297 | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL255950 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL270838 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL402893 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL410037 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL270568 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL270879 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL257203 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL403179 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL401864 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL402351 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL403761 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL270588 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL404160 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL257204 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL403921 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL257461 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL403172 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL272788 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL271428 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL272923 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL255843 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL255370 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL271019 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL270839 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL272789 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL438386 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL403178 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL411457 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL403966 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL403334 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL273141 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL415099 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL271054 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL273143 | — | Ki | = | 201.0 | nM | 6.70 |