Assay Detail
Binding
CHEMBL3382095
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| 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 | 35 | 6.48 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357142 | — | — | 1 | 8.70 |
| CHEMBL3357143 | — | — | 1 | 8.52 |
| CHEMBL3357141 | — | — | 1 | 8.52 |
| CHEMBL2010601 | IVACAFTOR | 4.0 | 1 | 8.52 |
| CHEMBL3356646 | — | — | 1 | 8.05 |
| CHEMBL3357126 | — | — | 1 | 7.96 |
| CHEMBL3357125 | — | — | 1 | 7.70 |
| CHEMBL3357139 | — | — | 1 | 7.00 |
| CHEMBL3354673 | — | — | 1 | 7.00 |
| CHEMBL3356645 | — | — | 1 | 7.00 |
| CHEMBL3357140 | — | — | 1 | 7.00 |
| CHEMBL3357132 | — | — | 1 | 7.00 |
| CHEMBL3357136 | — | — | 1 | 7.00 |
| CHEMBL3356627 | — | — | 1 | 6.70 |
| CHEMBL3356632 | — | — | 1 | 6.70 |
| CHEMBL3356630 | — | — | 1 | 6.70 |
| CHEMBL3357130 | — | — | 1 | 6.52 |
| CHEMBL3357131 | — | — | 1 | 6.40 |
| CHEMBL3356635 | — | — | 1 | 6.40 |
| CHEMBL3356631 | — | — | 1 | 6.10 |
| CHEMBL3356633 | — | — | 1 | 6.10 |
| CHEMBL3356626 | — | — | 1 | 5.89 |
| CHEMBL3356629 | — | — | 1 | 5.82 |
| CHEMBL3357129 | — | — | 1 | 5.77 |
| CHEMBL3354672 | — | — | 1 | 5.68 |
| CHEMBL3357134 | — | — | 1 | 5.46 |
| CHEMBL3356625 | — | — | 1 | 5.46 |
| CHEMBL3357138 | — | — | 1 | 5.29 |
| CHEMBL3356638 | — | — | 1 | 5.25 |
| CHEMBL3357128 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357142 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3357143 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2010601 | IVACAFTOR | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3357141 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3356646 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3357126 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3357125 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3357139 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3354673 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3356645 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3357140 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3357132 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3357136 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3356630 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3356632 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3356627 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3357130 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3357131 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3356635 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3356631 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3356633 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3356626 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3356629 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3357129 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3354672 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3356625 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3357134 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3357138 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3356638 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3357128 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3356634 | — | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3356636 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3357127 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3356628 | — | EC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL3356621 | — | EC50 | = | 16000.0 | nM | 4.80 |