Assay Detail
Binding
CHEMBL3870967
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
The discovery of quinoline based single-ligand human H1 and H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.32 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1767164 | GSK-1004723 | 2.0 | 1 | 7.30 |
| CHEMBL639 | AZELASTINE | 4.0 | 1 | 7.00 |
| CHEMBL3921827 | — | — | 1 | 6.00 |
| CHEMBL3893197 | — | — | 1 | 5.80 |
| CHEMBL3898341 | — | — | 1 | 5.60 |
| CHEMBL3917428 | — | — | 1 | 5.20 |
| CHEMBL3947980 | — | — | 1 | 5.10 |
| CHEMBL3935303 | — | — | 1 | 4.80 |
| CHEMBL3967709 | — | — | 1 | 4.70 |
| CHEMBL3925977 | — | — | 1 | 4.50 |
| CHEMBL3907368 | — | — | 1 | 4.50 |
| CHEMBL3925332 | — | — | 1 | 4.40 |
| CHEMBL3926412 | — | — | 1 | 4.30 |
| CHEMBL3896541 | — | — | 1 | - |
| CHEMBL3953018 | — | — | 1 | - |
| CHEMBL3952802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1767164 | GSK-1004723 | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL639 | AZELASTINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3921827 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3893197 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3898341 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3917428 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3947980 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3935303 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3967709 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL3925977 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3907368 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3925332 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3926412 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3896541 | — | IC50 | > | 63095.73 | nM | - |
| CHEMBL3953018 | — | IC50 | > | 63095.73 | nM | - |
| CHEMBL3952802 | — | IC50 | > | 63095.73 | nM | - |