Assay Detail
Binding
CHEMBL4022897
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Corrector activity at CFTR F508del/F508del mutant in primary HBE cells assessed as increase in chloride ion current across apical membrane measured 18 to 24 hrs post compound treatment on basolateral side of cells in presence of channel potentiator GLPG1837 by trans-epithelial current clamp method
10
Total Activities
10
Compounds Tested
2
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 | 9 | 7.16 | 8.30 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4101487 | GALICAFTOR | 2.0 | 1 | 8.30 |
| CHEMBL4066196 | — | — | 1 | 8.05 |
| CHEMBL4093612 | A-1596586 | — | 1 | 7.55 |
| CHEMBL4093771 | — | — | 1 | 7.12 |
| CHEMBL4067042 | — | — | 1 | 7.06 |
| CHEMBL4077999 | — | — | 1 | 6.96 |
| CHEMBL4096042 | — | — | 1 | 6.68 |
| CHEMBL4085871 | — | — | 1 | 6.62 |
| CHEMBL4094248 | — | — | 1 | 6.12 |
| CHEMBL2103870 | LUMACAFTOR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4101487 | GALICAFTOR | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4066196 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4093612 | A-1596586 | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4093771 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4067042 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4077999 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4096042 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4085871 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4094248 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2103870 | LUMACAFTOR | Activity | - | — | - |