Assay Detail
Binding
CHEMBL4022894
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Corrector activity at HRP-fused CFTR F508del mutant (unknown origin) expressed in human CFBE41o cells assessed as increase in matured protein levels at cell surface after 18 to 24 hrs by luminescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 5.90 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093612 | A-1596586 | — | 1 | 6.89 |
| CHEMBL4101344 | — | — | 1 | 6.70 |
| CHEMBL4085871 | — | — | 1 | 6.64 |
| CHEMBL4074654 | — | — | 1 | 6.35 |
| CHEMBL4102835 | — | — | 1 | 6.03 |
| CHEMBL4066040 | A-1596584 | — | 1 | 6.00 |
| CHEMBL4094248 | — | — | 1 | 5.80 |
| CHEMBL4083915 | — | — | 1 | 5.64 |
| CHEMBL4086410 | — | — | 1 | 5.60 |
| CHEMBL4073541 | — | — | 1 | 5.60 |
| CHEMBL4091682 | — | — | 1 | 5.57 |
| CHEMBL4078555 | — | — | 1 | 5.41 |
| CHEMBL4094173 | — | — | 1 | 5.37 |
| CHEMBL4064946 | — | — | 1 | 4.96 |
| CHEMBL4101906 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093612 | A-1596586 | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4101344 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4085871 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4074654 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4102835 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4066040 | A-1596584 | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4094248 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4083915 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4086410 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4073541 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4091682 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4078555 | — | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4094173 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4064946 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4101906 | — | EC50 | > | 20000.0 | nM | - |