Assay Detail
Binding
CHEMBL1781191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay
57
Total Activities
57
Compounds Tested
1
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
Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 6.47 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1780061 | — | — | 1 | 8.52 |
| CHEMBL507974 | TETRODOTOXIN | 3.0 | 1 | 8.22 |
| CHEMBL1779935 | — | — | 1 | 7.70 |
| CHEMBL1780051 | — | — | 1 | 7.52 |
| CHEMBL1779936 | — | — | 1 | 7.52 |
| CHEMBL1779938 | — | — | 1 | 7.40 |
| CHEMBL1779937 | — | — | 1 | 7.40 |
| CHEMBL1779941 | — | — | 1 | 7.22 |
| CHEMBL1779940 | — | — | 1 | 7.22 |
| CHEMBL1779939 | — | — | 1 | 7.22 |
| CHEMBL1779943 | — | — | 1 | 7.16 |
| CHEMBL1779942 | — | — | 1 | 7.16 |
| CHEMBL1780035 | — | — | 1 | 7.10 |
| CHEMBL1780037 | — | — | 1 | 7.05 |
| CHEMBL1780036 | — | — | 1 | 7.05 |
| CHEMBL1780038 | — | — | 1 | 6.96 |
| CHEMBL1780039 | — | — | 1 | 6.89 |
| CHEMBL1780040 | — | — | 1 | 6.85 |
| CHEMBL1779921 | — | — | 1 | 6.70 |
| CHEMBL1779923 | — | — | 1 | 6.70 |
| CHEMBL1780041 | — | — | 1 | 6.66 |
| CHEMBL1779924 | — | — | 1 | 6.57 |
| CHEMBL1779920 | — | — | 1 | 6.52 |
| CHEMBL1780062 | — | — | 1 | 6.36 |
| CHEMBL1779925 | — | — | 1 | 6.32 |
| CHEMBL1780045 | — | — | 1 | 6.20 |
| CHEMBL1780050 | — | — | 1 | 5.96 |
| CHEMBL1780064 | — | — | 1 | 5.93 |
| CHEMBL1779926 | — | — | 1 | 5.92 |
| CHEMBL1780063 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1780061 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL507974 | TETRODOTOXIN | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1779935 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1780051 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1779936 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1779938 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1779937 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1779941 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1779940 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1779939 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1779943 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1779942 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1780035 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1780036 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1780037 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1780038 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1780039 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1780040 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1779921 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1779923 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1780041 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1779924 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1779920 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1780062 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1779925 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1780045 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1780050 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1780064 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL1779926 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL1780063 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL1779927 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL1780047 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL1780044 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL1780060 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL1780048 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1780042 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL1779928 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL1780059 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL1779929 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL1779930 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL1779922 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL1779931 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL1779932 | — | IC50 | = | 7370.0 | nM | 5.13 |
| CHEMBL698 | TETRACAINE | IC50 | = | 7510.0 | nM | 5.12 |
| CHEMBL1780046 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1780058 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1780057 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1780056 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1780055 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1780054 | — | IC50 | > | 5000.0 | nM | - |