Assay Detail
Binding
CHEMBL2330781
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG K+ channel expressed in HEK293 cells by scintillation spectrophotometric analysis
42
Total Activities
42
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.59 | 8.39 |
| IC60 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 8.39 |
| CHEMBL2324254 | — | — | 1 | 8.29 |
| CHEMBL2324257 | — | — | 1 | 8.00 |
| CHEMBL2324244 | — | — | 1 | 7.85 |
| CHEMBL2325208 | — | — | 1 | 7.82 |
| CHEMBL2325204 | — | — | 1 | 7.62 |
| CHEMBL2325199 | — | — | 1 | 7.62 |
| CHEMBL2325200 | — | — | 1 | 7.40 |
| CHEMBL2324262 | — | — | 1 | 7.28 |
| CHEMBL2324245 | — | — | 1 | 7.22 |
| CHEMBL2324246 | — | — | 1 | 7.13 |
| CHEMBL2324247 | — | — | 1 | 7.13 |
| CHEMBL2325205 | — | — | 1 | 7.07 |
| CHEMBL2324263 | — | — | 1 | 6.97 |
| CHEMBL2324264 | — | — | 1 | 6.87 |
| CHEMBL2324243 | — | — | 1 | 6.80 |
| CHEMBL2324256 | — | — | 1 | 6.77 |
| CHEMBL2324242 | — | — | 1 | 6.68 |
| CHEMBL2325201 | — | — | 1 | 6.54 |
| CHEMBL2325212 | — | — | 1 | 6.53 |
| CHEMBL2324261 | — | — | 1 | 6.46 |
| CHEMBL2325206 | — | — | 1 | 6.43 |
| CHEMBL2325213 | — | — | 1 | 6.42 |
| CHEMBL2324251 | — | — | 1 | 6.33 |
| CHEMBL2325210 | — | — | 1 | 6.26 |
| CHEMBL2324248 | — | — | 1 | 6.12 |
| CHEMBL2325214 | — | — | 1 | 5.94 |
| CHEMBL2324250 | — | — | 1 | 5.79 |
| CHEMBL2325207 | — | — | 1 | 5.70 |
| CHEMBL2325209 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2324254 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2324257 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2324244 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2325208 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2325204 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2325199 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2325200 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2324262 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2324245 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2324246 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2324247 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2325205 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2324263 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2324264 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2324243 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2324256 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2324242 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL2325201 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL2325212 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL2324261 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL2325206 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL2325213 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL2324251 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL2325210 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL2324248 | — | IC50 | = | 767.0 | nM | 6.12 |
| CHEMBL2325214 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL2324250 | — | IC50 | = | 1608.0 | nM | 5.79 |
| CHEMBL2325207 | — | IC50 | = | 1992.0 | nM | 5.70 |
| CHEMBL2325209 | — | IC50 | = | 2908.0 | nM | 5.54 |
| CHEMBL2325216 | — | IC50 | = | 3901.0 | nM | 5.41 |
| CHEMBL2325215 | — | IC50 | = | 4019.0 | nM | 5.40 |
| CHEMBL2325211 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL2325217 | — | IC50 | = | 14014.0 | nM | 4.85 |
| CHEMBL2325203 | — | IC50 | = | 14426.0 | nM | 4.84 |
| CHEMBL2324239 | — | IC50 | = | 31077.0 | nM | 4.51 |
| CHEMBL2325202 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324255 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2324258 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL2324259 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL2324260 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL2324237 | — | IC60 | > | 10.0 | uM | - |