Assay Detail
Binding
CHEMBL869626
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against human hERG receptor expressed in HEK cells
11
Total Activities
11
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 | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.97 | 5.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206115 | — | — | 1 | 5.25 |
| CHEMBL206249 | — | — | 1 | 5.18 |
| CHEMBL378547 | — | — | 1 | 5.11 |
| CHEMBL262736 | — | — | 1 | 5.11 |
| CHEMBL381526 | — | — | 1 | 5.07 |
| CHEMBL206798 | — | — | 1 | 4.82 |
| CHEMBL377596 | — | — | 1 | 4.75 |
| CHEMBL381533 | — | — | 1 | 4.48 |
| CHEMBL439342 | — | — | 1 | - |
| CHEMBL382994 | — | — | 1 | - |
| CHEMBL202734 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206115 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL206249 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL378547 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL262736 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL381526 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL206798 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL377596 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL381533 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL439342 | — | IC50 | - | — | - | |
| CHEMBL382994 | — | IC50 | - | — | - | |
| CHEMBL202734 | — | IC50 | - | — | - |