Assay Detail
Binding
CHEMBL3385212
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Epithelial cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.56 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357141 | — | — | 1 | 8.30 |
| CHEMBL3357143 | — | — | 1 | 7.66 |
| CHEMBL2010601 | IVACAFTOR | 4.0 | 1 | 7.66 |
| CHEMBL3356646 | — | — | 1 | 7.38 |
| CHEMBL3357142 | — | — | 1 | 7.35 |
| CHEMBL3357126 | — | — | 1 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357141 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3357143 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2010601 | IVACAFTOR | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3356646 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3357142 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3357126 | — | EC50 | = | 97.0 | nM | 7.01 |