Assay Detail
Binding
CHEMBL2019763
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Blockade of human ENaC expressed in HBE cells by short-circuit current assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HBE |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 2: α-Branched quaternary amines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.64 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212432 | 552-02 FREE BASE | 2.0 | 1 | 8.70 |
| CHEMBL2017996 | — | — | 1 | 8.40 |
| CHEMBL2017991 | — | — | 1 | 7.52 |
| CHEMBL2017994 | — | — | 1 | 7.23 |
| CHEMBL2017995 | — | — | 1 | 6.77 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 6.66 |
| CHEMBL2017990 | — | — | 1 | 6.54 |
| CHEMBL2017988 | — | — | 1 | 6.29 |
| CHEMBL2017989 | — | — | 1 | 6.12 |
| CHEMBL2017993 | — | — | 1 | 5.62 |
| CHEMBL2017986 | — | — | 1 | 5.09 |
| CHEMBL2017992 | — | — | 1 | 4.71 |
| CHEMBL2017985 | — | — | 1 | - |
| CHEMBL2017987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212432 | 552-02 FREE BASE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2017996 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2017991 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2017994 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2017995 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL945 | AMILORIDE | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2017990 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2017988 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2017989 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2017993 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL2017986 | — | IC50 | = | 8090.0 | nM | 5.09 |
| CHEMBL2017992 | — | IC50 | = | 19510.0 | nM | 4.71 |
| CHEMBL2017985 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2017987 | — | IC50 | > | 30000.0 | nM | - |