Assay Detail
Functional
CHEMBL2013637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NaV1.5 channel by patchXpress assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗| 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 |
|---|---|---|---|
| IC50 | 39 | 6.85 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012259 | — | — | 1 | 7.70 |
| CHEMBL2012299 | — | — | 1 | 7.70 |
| CHEMBL2012180 | — | — | 1 | 7.52 |
| CHEMBL2012298 | — | — | 1 | 7.52 |
| CHEMBL2012292 | — | — | 1 | 7.40 |
| CHEMBL2012274 | — | — | 1 | 7.40 |
| CHEMBL2012273 | — | — | 1 | 7.40 |
| CHEMBL2012179 | — | — | 1 | 7.30 |
| CHEMBL2012272 | — | — | 1 | 7.30 |
| CHEMBL2012291 | — | — | 1 | 7.22 |
| CHEMBL2012266 | — | — | 1 | 7.22 |
| CHEMBL2012271 | — | — | 1 | 7.16 |
| CHEMBL2012285 | — | — | 1 | 7.10 |
| CHEMBL2012300 | — | — | 1 | 7.10 |
| CHEMBL2012181 | — | — | 1 | 7.10 |
| CHEMBL2012290 | — | — | 1 | 7.05 |
| CHEMBL2012296 | — | — | 1 | 7.05 |
| CHEMBL2012262 | — | — | 1 | 6.96 |
| CHEMBL2012295 | — | — | 1 | 6.96 |
| CHEMBL2012178 | — | — | 1 | 6.92 |
| CHEMBL2012268 | — | — | 1 | 6.92 |
| CHEMBL2012250 | — | — | 1 | 6.89 |
| CHEMBL2012265 | — | — | 1 | 6.85 |
| CHEMBL2012293 | — | — | 1 | 6.82 |
| CHEMBL2012287 | — | — | 1 | 6.80 |
| CHEMBL2012269 | — | — | 1 | 6.72 |
| CHEMBL2012301 | — | — | 1 | 6.72 |
| CHEMBL2012244 | — | — | 1 | 6.70 |
| CHEMBL2012249 | — | — | 1 | 6.60 |
| CHEMBL2012263 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012259 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2012299 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2012298 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2012180 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2012292 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2012274 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2012273 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2012179 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2012272 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2012291 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2012266 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2012271 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2012285 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2012300 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2012181 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2012290 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2012296 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2012262 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2012295 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2012178 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2012268 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2012250 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2012265 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2012293 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2012287 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2012269 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2012301 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2012244 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2012249 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2012263 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2012245 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2012283 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2012294 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2012281 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2012277 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL2012247 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL2012246 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL2012267 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2012280 | — | IC50 | = | 2700.0 | nM | 5.57 |