Assay Detail
Binding
CHEMBL984535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells
23
Total Activities
23
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
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.94 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL456171 | — | — | 1 | 6.70 |
| CHEMBL499477 | — | — | 1 | 6.17 |
| CHEMBL514564 | — | — | 1 | 6.13 |
| CHEMBL485547 | — | — | 1 | 6.02 |
| CHEMBL456808 | — | — | 1 | 5.57 |
| CHEMBL464804 | — | — | 1 | 5.16 |
| CHEMBL519193 | — | — | 1 | 5.05 |
| CHEMBL484931 | — | — | 1 | 4.87 |
| CHEMBL521509 | — | — | 1 | 4.78 |
| CHEMBL484754 | — | — | 1 | 4.73 |
| CHEMBL484753 | — | — | 1 | 4.64 |
| CHEMBL464600 | — | — | 1 | 4.50 |
| CHEMBL456172 | — | — | 1 | 4.50 |
| CHEMBL519355 | — | — | 1 | 4.47 |
| CHEMBL520502 | — | — | 1 | 4.44 |
| CHEMBL372575 | — | — | 1 | 4.30 |
| CHEMBL485620 | — | — | 1 | 4.30 |
| CHEMBL485629 | MK-0873 | 2.0 | 1 | 4.18 |
| CHEMBL456173 | — | — | 1 | 4.15 |
| CHEMBL520463 | — | — | 1 | 4.05 |
| CHEMBL464803 | — | — | 1 | - |
| CHEMBL511368 | — | — | 1 | - |
| CHEMBL464802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL456171 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL499477 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL514564 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL485547 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL456808 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL464804 | — | IC50 | = | 6960.0 | nM | 5.16 |
| CHEMBL519193 | — | IC50 | = | 8950.0 | nM | 5.05 |
| CHEMBL484931 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL521509 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL484754 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL484753 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL464600 | — | IC50 | = | 31800.0 | nM | 4.50 |
| CHEMBL456172 | — | IC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL519355 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL520502 | — | IC50 | = | 36600.0 | nM | 4.44 |
| CHEMBL372575 | — | IC50 | = | 49900.0 | nM | 4.30 |
| CHEMBL485620 | — | IC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL485629 | MK-0873 | IC50 | = | 65700.0 | nM | 4.18 |
| CHEMBL456173 | — | IC50 | = | 71500.0 | nM | 4.15 |
| CHEMBL520463 | — | IC50 | = | 89400.0 | nM | 4.05 |
| CHEMBL464803 | — | IC50 | > | 94500.0 | nM | - |
| CHEMBL511368 | — | IC50 | - | — | - | |
| CHEMBL464802 | — | IC50 | - | — | - |