Assay Detail
Binding
CHEMBL956578
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]MK499 from human ERG expressed in HEK293 cells
19
Total Activities
19
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
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.70 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487059 | — | — | 1 | 6.77 |
| CHEMBL453894 | — | — | 1 | 6.46 |
| CHEMBL487060 | — | — | 1 | 6.34 |
| CHEMBL453893 | — | — | 1 | 5.96 |
| CHEMBL519067 | — | — | 1 | 5.77 |
| CHEMBL487230 | — | — | 1 | 5.75 |
| CHEMBL508712 | — | — | 1 | 5.70 |
| CHEMBL487064 | — | — | 1 | 5.55 |
| CHEMBL488248 | — | — | 1 | 5.54 |
| CHEMBL455681 | — | — | 1 | 5.54 |
| CHEMBL488251 | — | — | 1 | 5.52 |
| CHEMBL453654 | — | — | 1 | 5.42 |
| CHEMBL454879 | — | — | 1 | 5.37 |
| CHEMBL488249 | — | — | 1 | 5.25 |
| CHEMBL487063 | — | — | 1 | 5.10 |
| CHEMBL454642 | — | — | 1 | 5.10 |
| CHEMBL453653 | — | — | 1 | - |
| CHEMBL453892 | — | — | 1 | - |
| CHEMBL507360 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487059 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL453894 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL487060 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL453893 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL519067 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL487230 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL508712 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL487064 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL488248 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL455681 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL488251 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL453654 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL454879 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL488249 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL487063 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL454642 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL453653 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL453892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL507360 | — | IC50 | > | 10000.0 | nM | - |