Assay Detail
Binding
CHEMBL4768154
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiator activity at CFTR F508del mutant (unknown origin) expressed in CFBE41o cells assessed as increase in forskolin induced transepithelial short circuit current by Ussing chamber assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CFBE41o- |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting different binding sites in the CFTR structures allows to synergistically potentiate channel activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.60 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2010601 | IVACAFTOR | 4.0 | 1 | 7.93 |
| CHEMBL4788315 | — | — | 1 | 6.06 |
| CHEMBL4794876 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2010601 | IVACAFTOR | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4788315 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4794876 | — | EC50 | = | 1510.0 | nM | 5.82 |