Assay Detail
ADMET
CHEMBL3591516
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human Kv11.1 expressed in HEK293 cell membranes assessed as binding affinity constant by [3H]dofetilide competition association 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 |
|---|---|---|---|
| Kd | 46 | 7.06 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590463 | — | — | 1 | 9.36 |
| CHEMBL3590452 | — | — | 1 | 9.14 |
| CHEMBL3140084 | — | — | 1 | 8.92 |
| CHEMBL3590464 | — | — | 1 | 8.72 |
| CHEMBL3590446 | — | — | 1 | 8.52 |
| CHEMBL3590465 | — | — | 1 | 8.40 |
| CHEMBL2324244 | — | — | 1 | 8.21 |
| CHEMBL3590462 | — | — | 1 | 7.92 |
| CHEMBL3093959 | — | — | 1 | 7.80 |
| CHEMBL3590458 | — | — | 1 | 7.75 |
| CHEMBL3590445 | — | — | 1 | 7.70 |
| CHEMBL3590457 | — | — | 1 | 7.47 |
| CHEMBL3590456 | — | — | 1 | 7.44 |
| CHEMBL3590466 | — | — | 1 | 7.43 |
| CHEMBL3590447 | — | — | 1 | 7.39 |
| CHEMBL3590444 | — | — | 1 | 7.28 |
| CHEMBL3590470 | — | — | 1 | 7.22 |
| CHEMBL3590495 | — | — | 1 | 7.14 |
| CHEMBL3590453 | — | — | 1 | 7.07 |
| CHEMBL3093953 | — | — | 1 | 7.07 |
| CHEMBL3590501 | — | — | 1 | 7.00 |
| CHEMBL3590448 | — | — | 1 | 7.00 |
| CHEMBL3093972 | — | — | 1 | 7.00 |
| CHEMBL3590500 | — | — | 1 | 6.99 |
| CHEMBL3590499 | — | — | 1 | 6.98 |
| CHEMBL3590496 | — | — | 1 | 6.90 |
| CHEMBL3590450 | — | — | 1 | 6.88 |
| CHEMBL2325212 | — | — | 1 | 6.88 |
| CHEMBL3590497 | — | — | 1 | 6.87 |
| CHEMBL3590467 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590463 | — | Kd | = | 0.44 | nM | 9.36 |
| CHEMBL3590452 | — | Kd | = | 0.73 | nM | 9.14 |
| CHEMBL3140084 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL3590464 | — | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL3590446 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3590465 | — | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL2324244 | — | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL3590462 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL3093959 | — | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL3590458 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL3590445 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL3590457 | — | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL3590456 | — | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL3590466 | — | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL3590447 | — | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL3590444 | — | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL3590470 | — | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL3590495 | — | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL3590453 | — | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL3093953 | — | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL3590501 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL3590448 | — | Kd | = | 99.0 | nM | 7.00 |
| CHEMBL3093972 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL3590500 | — | Kd | = | 103.0 | nM | 6.99 |
| CHEMBL3590499 | — | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL3590496 | — | Kd | = | 125.0 | nM | 6.90 |
| CHEMBL3590450 | — | Kd | = | 132.0 | nM | 6.88 |
| CHEMBL2325212 | — | Kd | = | 132.0 | nM | 6.88 |
| CHEMBL3590497 | — | Kd | = | 135.0 | nM | 6.87 |
| CHEMBL3590467 | — | Kd | = | 153.0 | nM | 6.82 |
| CHEMBL3590494 | — | Kd | = | 203.0 | nM | 6.69 |
| CHEMBL3590451 | — | Kd | = | 247.0 | nM | 6.61 |
| CHEMBL3590449 | — | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL2325210 | — | Kd | = | 368.0 | nM | 6.43 |
| CHEMBL3590498 | — | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL3590455 | — | Kd | = | 591.0 | nM | 6.23 |
| CHEMBL3590460 | — | Kd | = | 637.0 | nM | 6.20 |
| CHEMBL2325211 | — | Kd | = | 1074.0 | nM | 5.97 |
| CHEMBL3590459 | — | Kd | = | 1188.0 | nM | 5.92 |
| CHEMBL1464333 | — | Kd | = | 1812.0 | nM | 5.74 |
| CHEMBL3590468 | — | Kd | = | 4258.0 | nM | 5.37 |
| CHEMBL3590454 | — | Kd | = | 5807.0 | nM | 5.24 |
| CHEMBL2324257 | — | Kd | = | 6631.0 | nM | 5.18 |
| CHEMBL2324239 | — | Kd | = | 8877.0 | nM | 5.05 |
| CHEMBL3590469 | — | Kd | - | — | - | |
| CHEMBL3590461 | — | Kd | = | 190546.0 | nM | - |