Assay Detail
Binding
CHEMBL2013639
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of dofetilide from human ERG
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.88 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012273 | — | — | 1 | 6.52 |
| CHEMBL2012301 | — | — | 1 | 6.50 |
| CHEMBL2012269 | — | — | 1 | 6.22 |
| CHEMBL2012300 | — | — | 1 | 6.17 |
| CHEMBL2012293 | — | — | 1 | 6.14 |
| CHEMBL2012266 | — | — | 1 | 6.03 |
| CHEMBL2012272 | — | — | 1 | 6.02 |
| CHEMBL2012291 | — | — | 1 | 6.01 |
| CHEMBL2012299 | — | — | 1 | 6.00 |
| CHEMBL2012246 | — | — | 1 | 6.00 |
| CHEMBL2012260 | — | — | 1 | 5.96 |
| CHEMBL2012295 | — | — | 1 | 5.96 |
| CHEMBL2012263 | — | — | 1 | 5.92 |
| CHEMBL2012277 | — | — | 1 | 5.92 |
| CHEMBL2012179 | — | — | 1 | 5.85 |
| CHEMBL2012259 | — | — | 1 | 5.82 |
| CHEMBL2012181 | — | — | 1 | 5.82 |
| CHEMBL2012298 | — | — | 1 | 5.75 |
| CHEMBL2012292 | — | — | 1 | 5.66 |
| CHEMBL2012274 | — | — | 1 | 5.64 |
| CHEMBL2012271 | — | — | 1 | 5.64 |
| CHEMBL2012290 | — | — | 1 | 5.62 |
| CHEMBL2012268 | — | — | 1 | 5.61 |
| CHEMBL2012178 | — | — | 1 | 5.60 |
| CHEMBL2012180 | — | — | 1 | 5.60 |
| CHEMBL2012267 | — | — | 1 | 5.56 |
| CHEMBL2012294 | — | — | 1 | 5.54 |
| CHEMBL2012265 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012273 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL2012301 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2012269 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL2012300 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL2012293 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL2012266 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL2012272 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL2012291 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL2012299 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2012246 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL2012260 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2012295 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2012263 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2012277 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2012179 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2012259 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2012181 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2012298 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL2012292 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL2012274 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL2012271 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL2012290 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL2012268 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL2012178 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2012180 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2012267 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL2012294 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL2012265 | — | Ki | = | 3200.0 | nM | 5.50 |