Assay Detail
Binding
CHEMBL816205
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-dofetilide to HEK cells stably expressing hERG voltage-gated IKr potassium channel Kv11.1
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 | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.10 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146233 | — | — | 1 | 7.70 |
| CHEMBL150210 | — | — | 1 | 7.16 |
| CHEMBL147431 | — | — | 1 | 6.96 |
| CHEMBL149429 | — | — | 1 | 6.82 |
| CHEMBL83894 | FANANSERIN | 2.0 | 1 | 6.70 |
| CHEMBL150220 | — | — | 1 | 6.25 |
| CHEMBL146595 | — | — | 1 | 6.24 |
| CHEMBL358075 | — | — | 1 | 6.15 |
| CHEMBL145939 | — | — | 1 | 6.00 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 5.96 |
| CHEMBL146144 | — | — | 1 | 5.92 |
| CHEMBL148058 | — | — | 1 | 5.89 |
| CHEMBL148280 | — | — | 1 | 5.75 |
| CHEMBL147048 | — | — | 1 | 5.72 |
| CHEMBL148565 | — | — | 1 | 5.60 |
| CHEMBL504699 | — | — | 1 | 5.40 |
| CHEMBL146998 | — | — | 1 | 5.40 |
| CHEMBL146620 | — | — | 1 | 5.17 |
| CHEMBL146485 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146233 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL150210 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL147431 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL149429 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL83894 | FANANSERIN | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL150220 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL146595 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL358075 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL145939 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL146144 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL148058 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL148280 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL147048 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL148565 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL504699 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL146998 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL146620 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL146485 | — | Ki | = | 7143.0 | nM | 5.15 |