Assay Detail
Functional
CHEMBL1219662
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
71
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | Huh-7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 71 | 6.85 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1215196 | — | — | 1 | 8.70 |
| CHEMBL1215486 | — | — | 1 | 8.40 |
| CHEMBL1215197 | — | — | 1 | 8.22 |
| CHEMBL1215487 | — | — | 1 | 8.15 |
| CHEMBL1215331 | PF-03882845 | 1.0 | 2 | 8.05 |
| CHEMBL1215198 | — | — | 1 | 7.89 |
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 7.89 |
| CHEMBL1215130 | — | — | 1 | 7.85 |
| CHEMBL1215409 | — | — | 1 | 7.82 |
| CHEMBL1215127 | — | — | 1 | 7.80 |
| CHEMBL1215408 | — | — | 1 | 7.68 |
| CHEMBL1215626 | — | — | 1 | 7.60 |
| CHEMBL1215627 | — | — | 1 | 7.58 |
| CHEMBL1215129 | — | — | 1 | 7.58 |
| CHEMBL1214839 | — | — | 1 | 7.51 |
| CHEMBL1215693 | — | — | 1 | 7.50 |
| CHEMBL1215625 | — | — | 1 | 7.41 |
| CHEMBL1215691 | — | — | 1 | 7.39 |
| CHEMBL1215330 | — | — | 1 | 7.39 |
| CHEMBL1215128 | — | — | 1 | 7.28 |
| CHEMBL1215126 | — | — | 1 | 7.27 |
| CHEMBL1214838 | — | — | 1 | 7.25 |
| CHEMBL1214841 | — | — | 1 | 7.25 |
| CHEMBL1215690 | — | — | 1 | 7.24 |
| CHEMBL1215556 | — | — | 1 | 7.19 |
| CHEMBL1215263 | — | — | 1 | 7.16 |
| CHEMBL1215199 | — | — | 1 | 7.10 |
| CHEMBL1215755 | — | — | 1 | 7.08 |
| CHEMBL1215485 | — | — | 1 | 7.05 |
| CHEMBL1214685 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1215196 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1215486 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1215197 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1215487 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1215331 | PF-03882845 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1215198 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1215130 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1215409 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1215127 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1215408 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1215331 | PF-03882845 | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1215626 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1215129 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1215627 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1214839 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1215693 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1215625 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1215330 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1215691 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1215128 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1215126 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1214838 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1214841 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1215690 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1215556 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1215263 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1215199 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1215755 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1215485 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1214685 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1215411 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL1215262 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1215624 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1215488 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1215052 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL1214688 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1215329 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL1214766 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL1215758 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL1214840 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL1215053 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL1214968 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1214971 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL1215689 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1215553 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL1214767 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL1215265 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL1215410 | — | IC50 | = | 720.0 | nM | 6.14 |