Assay Detail
Binding
CHEMBL3872103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at GR in human HepG2 cells assessed as inhibition of protein mediated-transcriptional activity by MMTV-promoter driven luciferase reporter gene assay
47
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.68 | 10.52 |
| Efficacy | 23 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3895181 | — | — | 2 | 10.52 |
| CHEMBL3933702 | — | — | 2 | 10.15 |
| CHEMBL3966490 | — | — | 2 | 9.40 |
| CHEMBL3907029 | — | — | 2 | 9.05 |
| CHEMBL3904106 | — | — | 2 | 8.85 |
| CHEMBL3927299 | — | — | 2 | 7.43 |
| CHEMBL3982975 | — | — | 2 | 7.08 |
| CHEMBL3956011 | — | — | 2 | 7.04 |
| CHEMBL3967119 | — | — | 2 | 6.34 |
| CHEMBL3928010 | — | — | 2 | 6.25 |
| CHEMBL3937406 | — | — | 2 | 6.20 |
| CHEMBL3891049 | — | — | 2 | 5.87 |
| CHEMBL3937005 | — | — | 2 | 5.63 |
| CHEMBL3969438 | — | — | 2 | - |
| CHEMBL3980320 | — | — | 2 | - |
| CHEMBL3954977 | — | — | 2 | - |
| CHEMBL3904225 | — | — | 1 | - |
| CHEMBL3910192 | — | — | 2 | - |
| CHEMBL3909248 | — | — | 2 | - |
| CHEMBL3964460 | — | — | 2 | - |
| CHEMBL3981243 | — | — | 2 | - |
| CHEMBL3890008 | — | — | 2 | - |
| CHEMBL3894105 | — | — | 2 | - |
| CHEMBL3983602 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3895181 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3933702 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3966490 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3907029 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3904106 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3927299 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3982975 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3956011 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3967119 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL3928010 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL3937406 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL3891049 | — | IC50 | = | 1357.0 | nM | 5.87 |
| CHEMBL3937005 | — | IC50 | = | 2349.0 | nM | 5.63 |
| CHEMBL3890008 | — | Efficacy | = | 55.0 | % | - |
| CHEMBL3891049 | — | Efficacy | = | 23.0 | % | - |
| CHEMBL3982975 | — | Efficacy | = | -0.7 | % | - |
| CHEMBL3933702 | — | Efficacy | = | 0.06 | % | - |
| CHEMBL3907029 | — | Efficacy | = | -0.3 | % | - |
| CHEMBL3904106 | — | Efficacy | = | 1.7 | % | - |
| CHEMBL3966490 | — | Efficacy | = | -0.1 | % | - |
| CHEMBL3954977 | — | Efficacy | = | 239.0 | % | - |
| CHEMBL3981243 | — | Efficacy | = | 73.0 | % | - |
| CHEMBL3964460 | — | Efficacy | = | 84.0 | % | - |
| CHEMBL3928010 | — | Efficacy | = | 1.4 | % | - |
| CHEMBL3927299 | — | Efficacy | = | 39.0 | % | - |
| CHEMBL3937005 | — | Efficacy | = | 74.0 | % | - |
| CHEMBL3909248 | — | Efficacy | = | 90.0 | % | - |
| CHEMBL3910192 | — | Efficacy | = | 96.0 | % | - |
| CHEMBL3980320 | — | Efficacy | = | 112.0 | % | - |
| CHEMBL3969438 | — | Efficacy | = | 85.0 | % | - |
| CHEMBL3910192 | — | IC50 | - | — | - | |
| CHEMBL3964460 | — | IC50 | - | — | - | |
| CHEMBL3894105 | — | IC50 | - | — | - | |
| CHEMBL3981243 | — | IC50 | - | — | - | |
| CHEMBL3904225 | — | IC50 | - | — | - | |
| CHEMBL3983602 | — | IC50 | - | — | - | |
| CHEMBL3954977 | — | IC50 | - | — | - | |
| CHEMBL3969438 | — | IC50 | - | — | - | |
| CHEMBL3980320 | — | IC50 | - | — | - | |
| CHEMBL3894105 | — | Efficacy | = | 30.6 | % | - |
| CHEMBL3909248 | — | IC50 | - | — | - | |
| CHEMBL3890008 | — | IC50 | - | — | - | |
| CHEMBL3967119 | — | Efficacy | = | 10.0 | % | - |
| CHEMBL3895181 | — | Efficacy | = | 57.0 | % | - |
| CHEMBL3937406 | — | Efficacy | = | 46.0 | % | - |
| CHEMBL3956011 | — | Efficacy | = | 36.0 | % | - |
| CHEMBL3983602 | — | Efficacy | = | 147.0 | % | - |