Assay Detail
Binding
CHEMBL5037009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of CFTR F508del mutant (unknown origin) expressed in CHO cells assessed as chloride transport by measuring membrane potential incubated for 5 to 30 mins in presence of forskolin by Quattro assay
33
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 33 | 6.74 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5076312 | — | — | 2 | 8.10 |
| CHEMBL5088607 | — | — | 1 | 8.05 |
| CHEMBL5087757 | — | — | 1 | 8.05 |
| CHEMBL5075860 | — | — | 1 | 8.00 |
| CHEMBL5075769 | — | — | 1 | 7.82 |
| CHEMBL5084140 | — | — | 1 | 7.82 |
| CHEMBL5082569 | — | — | 2 | 7.70 |
| CHEMBL5081202 | — | — | 1 | 7.64 |
| CHEMBL5088068 | — | — | 1 | 7.52 |
| CHEMBL5093146 | — | — | 1 | 7.40 |
| CHEMBL4650318 | ICENTICAFTOR | 2.0 | 1 | 7.33 |
| CHEMBL5082261 | — | — | 1 | 7.16 |
| CHEMBL5080252 | — | — | 1 | 7.11 |
| CHEMBL5071764 | — | — | 1 | 7.11 |
| CHEMBL5075105 | — | — | 2 | 6.96 |
| CHEMBL5079547 | — | — | 1 | 6.64 |
| CHEMBL5083308 | — | — | 1 | 6.62 |
| CHEMBL5085939 | — | — | 1 | 6.62 |
| CHEMBL5086285 | — | — | 1 | 6.60 |
| CHEMBL5076850 | — | — | 1 | 6.48 |
| CHEMBL5083598 | — | — | 1 | 6.44 |
| CHEMBL5091133 | — | — | 1 | 6.33 |
| CHEMBL1949980 | — | — | 1 | 5.90 |
| CHEMBL5085049 | — | — | 1 | 5.73 |
| CHEMBL5085731 | — | — | 1 | 5.42 |
| CHEMBL5085858 | — | — | 1 | 5.28 |
| CHEMBL5077730 | — | — | 1 | 5.23 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.07 |
| CHEMBL1493986 | METHYL ANTHRANILATE | — | 1 | 4.52 |
| CHEMBL5077005 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5076312 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5088607 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5087757 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5075860 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5075769 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5084140 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5082569 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5081202 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5088068 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5093146 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5076312 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5082569 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4650318 | ICENTICAFTOR | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5082261 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5080252 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5071764 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5075105 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5079547 | — | EC50 | = | 229.0 | nM | 6.64 |
| CHEMBL5083308 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5085939 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5086285 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5075105 | — | EC50 | = | 276.0 | nM | 6.56 |
| CHEMBL5076850 | — | EC50 | = | 329.0 | nM | 6.48 |
| CHEMBL5083598 | — | EC50 | = | 362.0 | nM | 6.44 |
| CHEMBL5091133 | — | EC50 | = | 462.0 | nM | 6.33 |
| CHEMBL1949980 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL5085049 | — | EC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5085731 | — | EC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL5085858 | — | EC50 | = | 5310.0 | nM | 5.28 |
| CHEMBL5077730 | — | EC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL44 | GENISTEIN | EC50 | = | 8480.0 | nM | 5.07 |
| CHEMBL1493986 | METHYL ANTHRANILATE | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL5077005 | — | EC50 | = | 30000.0 | nM | 4.52 |