Assay Detail
Binding
CHEMBL3419342
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Inhibition of human NaV1.7 at -140 mV holding potential by whole-cell patch clamp assay
70
Total Activities
70
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
Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 70 | 7.32 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3417041 | — | — | 1 | 8.80 |
| CHEMBL3416921 | — | — | 1 | 8.70 |
| CHEMBL3318132 | — | — | 1 | 8.52 |
| CHEMBL3416942 | — | — | 1 | 8.52 |
| CHEMBL3416946 | — | — | 1 | 8.40 |
| CHEMBL3417038 | — | — | 1 | 8.40 |
| CHEMBL3416926 | — | — | 1 | 8.40 |
| CHEMBL3416943 | — | — | 1 | 8.40 |
| CHEMBL3416933 | — | — | 1 | 8.40 |
| CHEMBL3416937 | — | — | 1 | 8.40 |
| CHEMBL3416944 | — | — | 1 | 8.30 |
| CHEMBL3416927 | — | — | 1 | 8.30 |
| CHEMBL3416923 | — | — | 1 | 8.30 |
| CHEMBL3416928 | — | — | 1 | 8.22 |
| CHEMBL3417035 | — | — | 1 | 8.10 |
| CHEMBL3417040 | — | — | 1 | 8.10 |
| CHEMBL3416931 | — | — | 1 | 8.10 |
| CHEMBL3416917 | — | — | 1 | 8.05 |
| CHEMBL3416922 | — | — | 1 | 8.05 |
| CHEMBL3416938 | — | — | 1 | 8.00 |
| CHEMBL3416886 | — | — | 1 | 8.00 |
| CHEMBL3417039 | — | — | 1 | 7.96 |
| CHEMBL3416940 | — | — | 1 | 7.89 |
| CHEMBL3416920 | — | — | 1 | 7.72 |
| CHEMBL3416934 | — | — | 1 | 7.72 |
| CHEMBL3416936 | — | — | 1 | 7.64 |
| CHEMBL3416925 | — | — | 1 | 7.62 |
| CHEMBL3416932 | — | — | 1 | 7.62 |
| CHEMBL3416924 | — | — | 1 | 7.60 |
| CHEMBL3416939 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3417041 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3416921 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3416942 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3318132 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3416946 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3417038 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3416926 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3416943 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3416933 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3416937 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3416944 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3416927 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3416923 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3416928 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3416931 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3417040 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3417035 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3416917 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3416922 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3416938 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3416886 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3417039 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3416940 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3416920 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3416934 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3416936 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3416932 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3416925 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3416924 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3416939 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3417036 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4524054 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3416945 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3416919 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3417037 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3416941 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3416935 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3416918 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3416930 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3416902 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3416890 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3416898 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3416901 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3416914 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3416897 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3416904 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3416899 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3416896 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3416900 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3416929 | — | IC50 | = | 236.0 | nM | 6.63 |