Assay Detail
Binding
CHEMBL4028145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GAL4-DBD fused MR ligand binding domain transfected in human Huh7 cells co-expressing GAL4-RE-Luc assessed as reduction in aldosterone-induced luciferase activity after 16 hrs in presence of serum by luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.54 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097160 | — | — | 1 | 7.62 |
| CHEMBL4086109 | — | — | 1 | 7.48 |
| CHEMBL2181928 | — | — | 1 | 7.36 |
| CHEMBL4064593 | — | — | 1 | 7.26 |
| CHEMBL4100538 | — | — | 1 | 7.01 |
| CHEMBL4078214 | — | — | 1 | 6.98 |
| CHEMBL4098088 | — | — | 1 | 6.60 |
| CHEMBL4079143 | — | — | 1 | 6.58 |
| CHEMBL4059632 | — | — | 1 | 6.45 |
| CHEMBL4082524 | — | — | 1 | 6.39 |
| CHEMBL4062345 | — | — | 1 | 6.23 |
| CHEMBL4062371 | — | — | 1 | 5.92 |
| CHEMBL4079083 | — | — | 1 | 5.71 |
| CHEMBL4071008 | — | — | 1 | 5.52 |
| CHEMBL4081584 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097160 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4086109 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2181928 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4064593 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4100538 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4078214 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4098088 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4079143 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL4059632 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL4082524 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4062345 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL4062371 | — | IC50 | = | 1217.0 | nM | 5.92 |
| CHEMBL4079083 | — | IC50 | = | 1969.0 | nM | 5.71 |
| CHEMBL4071008 | — | IC50 | = | 2992.0 | nM | 5.52 |
| CHEMBL4081584 | — | IC50 | = | 10000.0 | nM | 5.00 |