Assay Detail
Binding
CHEMBL5037013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of wild-type CFTR (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | FRT |
| 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 Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.14 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084140 | — | — | 1 | 7.37 |
| CHEMBL2010601 | IVACAFTOR | 4.0 | 1 | 7.16 |
| CHEMBL4650318 | ICENTICAFTOR | 2.0 | 1 | 6.95 |
| CHEMBL1949980 | — | — | 1 | 6.00 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 4.85 |
| CHEMBL5080252 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084140 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2010601 | IVACAFTOR | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4650318 | ICENTICAFTOR | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL1949980 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL44 | GENISTEIN | EC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL5080252 | — | EC50 | = | 30000.0 | nM | 4.52 |