Assay Detail
Binding
CHEMBL5731677
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Chamber Electrophysiology Assay of CFTR Potentiation in CF Bronchial Epithelial Cells: Primary cystic fibrosis human bronchial epithelial (CF hBE) cells were expanded and cultured according to published methods (Neuberger et al., Ch. 4 of Cystic Fibrosis, Methods in Molecular Biology vol. 741, pp. 39-54 (2011)). Well-differentiated cells (>30 days at air/liquid interface) on Snapwell filters (Corning Costar, cat. no. 3801) were mounted in Ussing chambers (Physiologic Instruments, Inc., San Diego, Calif.). F508del/F508del cultures were assayed at 27° C. and G551D/F508del cells were assayed at 35° C. HEPES buffered physiological saline (composition (in mM): 137 NaCl, 4 KCl, 1 MgCl2, 1.8 CaCl2, 10 HEPES Na) was used in both apical and basolateral chambers. Chambers were bubbled with air to promote mixing and the voltage was clamped to zero. Amiloride (30 uM), forskolin (10 uM), test compound (4 increasing concentrations), and CFTRinh-172 (20 uM) were added sequentially with 20-25 minutes between additions. Short-circuit currents were acquired and analyzed using LabScribe2. Test compound responses were scaled relative to responses for DMSO (0%) and the maximal response of a positive control potentiator (100%).
165
Total Activities
36
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclic heteroaryl derivatives as CFTR potentiators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 55 | 7.95 | 9.70 |
| kon | 55 | - | - |
| k_off | 55 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5863288 | — | — | 6 | 9.70 |
| CHEMBL5861582 | — | — | 3 | 9.40 |
| CHEMBL5892004 | — | — | 6 | 9.38 |
| CHEMBL6033456 | — | — | 6 | 9.38 |
| CHEMBL5881985 | — | — | 3 | 9.18 |
| CHEMBL6009312 | — | — | 3 | 9.07 |
| CHEMBL5802461 | — | — | 3 | 8.98 |
| CHEMBL5860580 | — | — | 6 | 8.81 |
| CHEMBL5889215 | — | — | 6 | 8.78 |
| CHEMBL6000653 | — | — | 9 | 8.70 |
| CHEMBL5869365 | — | — | 6 | 8.70 |
| CHEMBL5964878 | — | — | 9 | 8.52 |
| CHEMBL5811687 | — | — | 3 | 8.41 |
| CHEMBL5974038 | — | — | 3 | 8.40 |
| CHEMBL5962153 | — | — | 6 | 8.26 |
| CHEMBL5989702 | — | — | 6 | 8.19 |
| CHEMBL5943989 | — | — | 6 | 8.16 |
| CHEMBL5963315 | — | — | 6 | 8.13 |
| CHEMBL5862902 | — | — | 3 | 8.05 |
| CHEMBL6053005 | — | — | 6 | 8.00 |
| CHEMBL5776338 | — | — | 3 | 7.98 |
| CHEMBL5963506 | — | — | 6 | 7.95 |
| CHEMBL5964959 | — | — | 3 | 7.89 |
| CHEMBL5792842 | — | — | 6 | 7.84 |
| CHEMBL5777022 | — | — | 3 | 7.80 |
| CHEMBL6006507 | — | — | 6 | 7.71 |
| CHEMBL6021895 | — | — | 3 | 7.70 |
| CHEMBL5923614 | — | — | 3 | 7.57 |
| CHEMBL5876993 | — | — | 3 | 7.55 |
| CHEMBL5825851 | — | — | 3 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5863288 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5861582 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL6033456 | — | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5892004 | — | EC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5881985 | — | EC50 | = | 0.66 | nM | 9.18 |
| CHEMBL6009312 | — | EC50 | = | 0.86 | nM | 9.07 |
| CHEMBL5802461 | — | EC50 | = | 1.05 | nM | 8.98 |
| CHEMBL5860580 | — | EC50 | = | 1.53 | nM | 8.81 |
| CHEMBL5889215 | — | EC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5869365 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6000653 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5863288 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5892004 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5964878 | — | EC50 | = | 3.02 | nM | 8.52 |
| CHEMBL5811687 | — | EC50 | = | 3.87 | nM | 8.41 |
| CHEMBL5974038 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6033456 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6000653 | — | EC50 | = | 4.93 | nM | 8.31 |
| CHEMBL5889215 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5962153 | — | EC50 | = | 5.48 | nM | 8.26 |
| CHEMBL5989702 | — | EC50 | = | 6.48 | nM | 8.19 |
| CHEMBL5943989 | — | EC50 | = | 6.96 | nM | 8.16 |
| CHEMBL5963315 | — | EC50 | = | 7.48 | nM | 8.13 |
| CHEMBL5964878 | — | EC50 | = | 7.86 | nM | 8.11 |
| CHEMBL5862902 | — | EC50 | = | 8.94 | nM | 8.05 |
| CHEMBL6053005 | — | EC50 | = | 9.95 | nM | 8.00 |
| CHEMBL5776338 | — | EC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5963506 | — | EC50 | = | 11.2 | nM | 7.95 |
| CHEMBL5964959 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5792842 | — | EC50 | = | 14.6 | nM | 7.84 |
| CHEMBL5777022 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6006507 | — | EC50 | = | 19.3 | nM | 7.71 |
| CHEMBL6021895 | — | EC50 | = | 19.8 | nM | 7.70 |
| CHEMBL5964878 | — | EC50 | = | 20.5 | nM | 7.69 |
| CHEMBL5792842 | — | EC50 | = | 20.9 | nM | 7.68 |
| CHEMBL5923614 | — | EC50 | = | 27.1 | nM | 7.57 |
| CHEMBL5876993 | — | EC50 | = | 28.4 | nM | 7.55 |
| CHEMBL5825851 | — | EC50 | = | 29.2 | nM | 7.54 |
| CHEMBL5860580 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5954441 | — | EC50 | = | 31.5 | nM | 7.50 |
| CHEMBL5962153 | — | EC50 | = | 33.5 | nM | 7.47 |
| CHEMBL6000653 | — | EC50 | = | 36.6 | nM | 7.44 |
| CHEMBL5943989 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5963506 | — | EC50 | = | 51.1 | nM | 7.29 |
| CHEMBL6024579 | — | EC50 | = | 74.4 | nM | 7.13 |
| CHEMBL6053005 | — | EC50 | = | 73.7 | nM | 7.13 |
| CHEMBL5869365 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5741266 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5961016 | — | EC50 | = | 123.0 | nM | 6.91 |
| CHEMBL5769135 | — | EC50 | = | 147.0 | nM | 6.83 |