Assay Detail
Binding
CHEMBL1648563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]N-[(4R)-10-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,40-piperidin]-6-yl]methanesulfonamide from human ERG expressed in HEK293 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.48 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1642479 | — | — | 1 | 9.17 |
| CHEMBL1642487 | — | — | 1 | 9.09 |
| CHEMBL1642476 | — | — | 1 | 8.92 |
| CHEMBL1642493 | — | — | 1 | 8.77 |
| CHEMBL1642475 | — | — | 1 | 8.77 |
| CHEMBL1642474 | — | — | 1 | 8.72 |
| CHEMBL1642477 | — | — | 1 | 8.62 |
| CHEMBL1642472 | — | — | 1 | 8.54 |
| CHEMBL1642471 | — | — | 1 | 8.37 |
| CHEMBL1642486 | — | — | 1 | 8.37 |
| CHEMBL1642482 | — | — | 1 | 8.24 |
| CHEMBL1642490 | — | — | 1 | 8.24 |
| CHEMBL1642492 | — | — | 1 | 8.15 |
| CHEMBL1641614 | — | — | 1 | 8.09 |
| CHEMBL584538 | — | — | 1 | 8.05 |
| CHEMBL1642491 | — | — | 1 | 8.03 |
| CHEMBL1642485 | — | — | 1 | 8.01 |
| CHEMBL1642470 | — | — | 1 | - |
| CHEMBL1642494 | — | — | 1 | - |
| CHEMBL1642489 | — | — | 1 | - |
| CHEMBL1642488 | — | — | 1 | - |
| CHEMBL1642484 | — | — | 1 | - |
| CHEMBL1642468 | — | — | 1 | - |
| CHEMBL1642478 | — | — | 1 | - |
| CHEMBL1642473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1642479 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL1642487 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL1642476 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1642493 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1642475 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1642474 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1642477 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1642472 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1642471 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1642486 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1642482 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1642490 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1642492 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1641614 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL584538 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1642491 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1642485 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL1642470 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL1642494 | — | IC50 | - | — | - | |
| CHEMBL1642489 | — | IC50 | - | — | - | |
| CHEMBL1642488 | — | IC50 | - | — | - | |
| CHEMBL1642484 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL1642468 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL1642478 | — | IC50 | - | — | - | |
| CHEMBL1642473 | — | IC50 | - | — | - |