Assay Detail
Binding
CHEMBL5131017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of homozygous F508del/F508del CFTR mutant in HBE cells incubated for 18 to 24 hrs by trans-epithelial current clamp assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HBE |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel Substituted Cyclopropyl Compounds as CFTR Modulators for Treating Cystic Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 9.18 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178232 | — | — | 1 | 9.40 |
| CHEMBL5193680 | — | — | 1 | 9.29 |
| CHEMBL5178488 | — | — | 1 | 9.18 |
| CHEMBL5202275 | — | — | 1 | 9.10 |
| CHEMBL5186971 | — | — | 1 | 9.08 |
| CHEMBL5171054 | — | — | 1 | 9.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178232 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5193680 | — | EC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5178488 | — | EC50 | = | 0.66 | nM | 9.18 |
| CHEMBL5202275 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5186971 | — | EC50 | = | 0.84 | nM | 9.08 |
| CHEMBL5171054 | — | EC50 | = | 0.9 | nM | 9.05 |