Assay Detail
Binding
CHEMBL768699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from HEK cells expressing hERG voltage dependent IKr potassium channel Kv11.1
24
Total Activities
24
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
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.89 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113667 | — | — | 1 | 7.75 |
| CHEMBL40584 | — | — | 1 | 7.10 |
| CHEMBL496687 | — | — | 1 | 6.96 |
| CHEMBL46523 | — | — | 1 | 6.54 |
| CHEMBL496860 | — | — | 1 | 6.30 |
| CHEMBL44310 | — | — | 1 | 6.28 |
| CHEMBL497064 | — | — | 1 | 6.03 |
| CHEMBL296512 | — | — | 1 | 5.89 |
| CHEMBL498048 | — | — | 1 | 5.85 |
| CHEMBL497054 | — | — | 1 | 5.82 |
| CHEMBL523245 | — | — | 1 | 5.80 |
| CHEMBL523585 | — | — | 1 | 5.68 |
| CHEMBL523760 | — | — | 1 | 5.60 |
| CHEMBL498729 | — | — | 1 | 5.52 |
| CHEMBL504699 | — | — | 1 | 5.40 |
| CHEMBL42557 | — | — | 1 | 5.31 |
| CHEMBL507898 | — | — | 1 | 5.27 |
| CHEMBL295559 | — | — | 1 | 5.24 |
| CHEMBL43697 | — | — | 1 | 5.16 |
| CHEMBL507727 | — | — | 1 | 5.09 |
| CHEMBL43819 | — | — | 1 | 5.02 |
| CHEMBL497877 | — | — | 1 | - |
| CHEMBL497878 | — | — | 1 | - |
| CHEMBL496852 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113667 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL40584 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL496687 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL46523 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL496860 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL44310 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL497064 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL296512 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL498048 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL497054 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL523245 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL523585 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL523760 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL498729 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL504699 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL42557 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL507898 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL295559 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL43697 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL507727 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL43819 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL497877 | — | Ki | > | 1100.0 | nM | - |
| CHEMBL497878 | — | Ki | > | 7000.0 | nM | - |
| CHEMBL496852 | — | Ki | > | 7000.0 | nM | - |