Assay Detail
Binding
CHEMBL868533
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dog bronchi prototypical epithelial sodium channel by electrophysiological assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Amiloride-sensitive sodium channel subunit alpha (CHEMBL1791) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.40 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212431 | — | — | 1 | 8.15 |
| CHEMBL212531 | — | — | 1 | 8.15 |
| CHEMBL212432 | 552-02 FREE BASE | 2.0 | 1 | 8.10 |
| CHEMBL209303 | — | — | 1 | 8.05 |
| CHEMBL211161 | — | — | 1 | 8.05 |
| CHEMBL214239 | — | — | 1 | 7.85 |
| CHEMBL377986 | — | — | 1 | 7.82 |
| CHEMBL211600 | — | — | 1 | 7.77 |
| CHEMBL210876 | — | — | 1 | 7.77 |
| CHEMBL380011 | — | — | 1 | 7.70 |
| CHEMBL379433 | — | — | 1 | 7.70 |
| CHEMBL212410 | — | — | 1 | 7.68 |
| CHEMBL386222 | — | — | 1 | 7.68 |
| CHEMBL379756 | — | — | 1 | 7.66 |
| CHEMBL214220 | — | — | 1 | 7.60 |
| CHEMBL212534 | — | — | 1 | 7.58 |
| CHEMBL211658 | — | — | 1 | 7.55 |
| CHEMBL209659 | — | — | 1 | 7.54 |
| CHEMBL379066 | — | — | 1 | 7.52 |
| CHEMBL208889 | — | — | 1 | 7.51 |
| CHEMBL211946 | — | — | 1 | 7.50 |
| CHEMBL211773 | — | — | 1 | 7.39 |
| CHEMBL211072 | — | — | 1 | 7.38 |
| CHEMBL209017 | — | — | 1 | 7.32 |
| CHEMBL211664 | — | — | 1 | 7.30 |
| CHEMBL213175 | — | — | 1 | 7.29 |
| CHEMBL208620 | — | — | 1 | 7.24 |
| CHEMBL209977 | — | — | 1 | 7.21 |
| CHEMBL211221 | — | — | 1 | 7.19 |
| CHEMBL212579 | BENZAMIL | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212431 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL212531 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL212432 | 552-02 FREE BASE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL209303 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL211161 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL214239 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL377986 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL211600 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL210876 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL380011 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL379433 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL386222 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL212410 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL379756 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL214220 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL212534 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL211658 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL209659 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL379066 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL208889 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL211946 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL211773 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL211072 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL209017 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL211664 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL213175 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL208620 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL209977 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL211221 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL212579 | BENZAMIL | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL211611 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL377239 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL380393 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL209104 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL211793 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL210966 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL377688 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL210981 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL210967 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL211502 | PHENAMIL | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL210866 | — | IC50 | = | 477.0 | nM | 6.32 |
| CHEMBL945 | AMILORIDE | IC50 | = | 776.0 | nM | 6.11 |