Assay Detail
ADMET
CHEMBL3591513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from human Kv11.1 expressed in HEK293 cell membranes by competitive radioligand displacement assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 6.92 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590463 | — | — | 1 | 9.55 |
| CHEMBL3590452 | — | — | 1 | 8.80 |
| CHEMBL3140084 | — | — | 1 | 8.74 |
| CHEMBL3590465 | — | — | 1 | 8.47 |
| CHEMBL3590464 | — | — | 1 | 8.46 |
| CHEMBL3590446 | — | — | 1 | 8.38 |
| CHEMBL2324244 | — | — | 1 | 8.22 |
| CHEMBL3590462 | — | — | 1 | 7.92 |
| CHEMBL3590466 | — | — | 1 | 7.77 |
| CHEMBL3590445 | — | — | 1 | 7.62 |
| CHEMBL3093959 | — | — | 1 | 7.51 |
| CHEMBL3590444 | — | — | 1 | 7.33 |
| CHEMBL3590458 | — | — | 1 | 7.32 |
| CHEMBL3590456 | — | — | 1 | 7.27 |
| CHEMBL3590457 | — | — | 1 | 7.22 |
| CHEMBL3590470 | — | — | 1 | 7.20 |
| CHEMBL3590447 | — | — | 1 | 7.19 |
| CHEMBL3590453 | — | — | 1 | 7.18 |
| CHEMBL3590501 | — | — | 1 | 7.15 |
| CHEMBL2325212 | — | — | 1 | 7.07 |
| CHEMBL3093972 | — | — | 1 | 7.01 |
| CHEMBL3590467 | — | — | 1 | 6.97 |
| CHEMBL3093953 | — | — | 1 | 6.92 |
| CHEMBL3590495 | — | — | 1 | 6.91 |
| CHEMBL3590497 | — | — | 1 | 6.86 |
| CHEMBL3590500 | — | — | 1 | 6.82 |
| CHEMBL3590496 | — | — | 1 | 6.75 |
| CHEMBL3590448 | — | — | 1 | 6.69 |
| CHEMBL3590499 | — | — | 1 | 6.61 |
| CHEMBL3590450 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590463 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3590452 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3140084 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3590465 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3590464 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3590446 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL2324244 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3590462 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3590466 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3590445 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3093959 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL3590444 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL3590458 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL3590456 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3590457 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3590470 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL3590447 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3590453 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL3590501 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL2325212 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL3093972 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL3590467 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3093953 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL3590495 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL3590497 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL3590500 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL3590496 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL3590448 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL3590499 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL3590450 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL3590498 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL3590451 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL2325210 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL3590494 | — | Ki | = | 577.0 | nM | 6.24 |
| CHEMBL3590449 | — | Ki | = | 588.0 | nM | 6.23 |
| CHEMBL3590455 | — | Ki | = | 944.0 | nM | 6.03 |
| CHEMBL3590468 | — | Ki | = | 1179.0 | nM | 5.93 |
| CHEMBL2325211 | — | Ki | = | 1208.0 | nM | 5.92 |
| CHEMBL3590460 | — | Ki | = | 1196.0 | nM | 5.92 |
| CHEMBL2324239 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL3590459 | — | Ki | = | 3282.0 | nM | 5.48 |
| CHEMBL2324257 | — | Ki | = | 3654.0 | nM | 5.44 |
| CHEMBL1464333 | — | Ki | = | 5418.0 | nM | 5.27 |
| CHEMBL3590454 | — | Ki | = | 5571.0 | nM | 5.25 |
| CHEMBL3590461 | — | Ki | = | 36870.0 | nM | 4.43 |
| CHEMBL3590469 | — | Ki | > | 100000.0 | nM | - |