Assay Detail
Binding
CHEMBL5731678
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FRT Ion Flux Assay of F508del CFTR Potentiation: Fischer rat thyroid (FRT) cell lines stably expressing recombinant F508del V470 CFTR and halide-sensitive yellow fluorescent protein (Pedemonte et al., J. Clin. Invest. 115(9) 2564-71 (2005)) were seeded at 25,000 cells/well in 50 uL/well of culture medium into black-walled, clear bottom tissue-culture-treated 384-well plates (Corning, cat. no. 3712). After one day, the cells were pre-incubated at 27° C./5% CO2 for 16-24 hours. The cells were then washed with dPBS and treated with forskolin (20 uM) and test compound for 30 min by addition of 20 uL of compound dilution buffer (dPBS containing forskolin and test compound). Plates were loaded into FLIPR384 fluorescence imaging plate reader (Molecular Devices). After an initial fluorescence reading, iodide buffer (25 uL) (composition (in mM): 137 NaI, 1.5 K2PO4, 8.1 NaH2PO4, 2.7 KCl, 0.5 MgCl2, 1 CaCl2) was added and a second fluorescence reading was made after approximately 21 seconds. Data treatment involved division of the second fluorescence reading by the initial fluorescence reading, then scaling of the resulting normalized endpoint fluorescence with respect to the responses for DMSO (0%) and a positive control potentiator (100%).
159
Total Activities
34
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 | 53 | 7.72 | 9.39 |
| kon | 53 | - | - |
| k_off | 53 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5802461 | — | — | 3 | 9.39 |
| CHEMBL5863288 | — | — | 6 | 9.25 |
| CHEMBL5892004 | — | — | 6 | 9.25 |
| CHEMBL6009312 | — | — | 3 | 9.24 |
| CHEMBL6033456 | — | — | 6 | 9.21 |
| CHEMBL6000653 | — | — | 9 | 8.73 |
| CHEMBL5964878 | — | — | 6 | 8.67 |
| CHEMBL5889215 | — | — | 6 | 8.51 |
| CHEMBL5881985 | — | — | 3 | 8.50 |
| CHEMBL5869365 | — | — | 6 | 8.47 |
| CHEMBL5943989 | — | — | 6 | 8.38 |
| CHEMBL5974038 | — | — | 3 | 8.33 |
| CHEMBL5860580 | — | — | 6 | 8.32 |
| CHEMBL5962153 | — | — | 6 | 8.30 |
| CHEMBL5989702 | — | — | 6 | 8.13 |
| CHEMBL5963315 | — | — | 6 | 8.06 |
| CHEMBL5963506 | — | — | 6 | 8.04 |
| CHEMBL5792842 | — | — | 6 | 7.97 |
| CHEMBL5776338 | — | — | 3 | 7.85 |
| CHEMBL5964959 | — | — | 3 | 7.76 |
| CHEMBL6053005 | — | — | 6 | 7.75 |
| CHEMBL5777022 | — | — | 3 | 7.74 |
| CHEMBL5923614 | — | — | 3 | 7.63 |
| CHEMBL6021895 | — | — | 3 | 7.58 |
| CHEMBL6006507 | — | — | 6 | 7.53 |
| CHEMBL5862902 | — | — | 3 | 7.52 |
| CHEMBL5954441 | — | — | 6 | 7.50 |
| CHEMBL5825851 | — | — | 3 | 7.43 |
| CHEMBL5876993 | — | — | 3 | 7.38 |
| CHEMBL5769135 | — | — | 6 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5802461 | — | EC50 | = | 0.41 | nM | 9.39 |
| CHEMBL5863288 | — | EC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5892004 | — | EC50 | = | 0.56 | nM | 9.25 |
| CHEMBL6009312 | — | EC50 | = | 0.57 | nM | 9.24 |
| CHEMBL6033456 | — | EC50 | = | 0.62 | nM | 9.21 |
| CHEMBL6000653 | — | EC50 | = | 1.88 | nM | 8.73 |
| CHEMBL5964878 | — | EC50 | = | 2.13 | nM | 8.67 |
| CHEMBL5889215 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5881985 | — | EC50 | = | 3.13 | nM | 8.50 |
| CHEMBL5869365 | — | EC50 | = | 3.36 | nM | 8.47 |
| CHEMBL5943989 | — | EC50 | = | 4.17 | nM | 8.38 |
| CHEMBL5974038 | — | EC50 | = | 4.65 | nM | 8.33 |
| CHEMBL5860580 | — | EC50 | = | 4.76 | nM | 8.32 |
| CHEMBL5962153 | — | EC50 | = | 5.05 | nM | 8.30 |
| CHEMBL6000653 | — | EC50 | = | 5.83 | nM | 8.23 |
| CHEMBL5863288 | — | EC50 | = | 6.59 | nM | 8.18 |
| CHEMBL5989702 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5963315 | — | EC50 | = | 8.76 | nM | 8.06 |
| CHEMBL5963506 | — | EC50 | = | 9.14 | nM | 8.04 |
| CHEMBL5792842 | — | EC50 | = | 10.6 | nM | 7.97 |
| CHEMBL6033456 | — | EC50 | = | 12.5 | nM | 7.90 |
| CHEMBL5892004 | — | EC50 | = | 13.3 | nM | 7.88 |
| CHEMBL5889215 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL5776338 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5964959 | — | EC50 | = | 17.2 | nM | 7.76 |
| CHEMBL6053005 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5777022 | — | EC50 | = | 18.4 | nM | 7.74 |
| CHEMBL5923614 | — | EC50 | = | 23.3 | nM | 7.63 |
| CHEMBL6021895 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5792842 | — | EC50 | = | 28.7 | nM | 7.54 |
| CHEMBL6006507 | — | EC50 | = | 29.6 | nM | 7.53 |
| CHEMBL5862902 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5954441 | — | EC50 | = | 31.8 | nM | 7.50 |
| CHEMBL5964878 | — | EC50 | = | 35.8 | nM | 7.45 |
| CHEMBL5825851 | — | EC50 | = | 37.2 | nM | 7.43 |
| CHEMBL5876993 | — | EC50 | = | 41.2 | nM | 7.38 |
| CHEMBL5962153 | — | EC50 | = | 45.2 | nM | 7.34 |
| CHEMBL5963506 | — | EC50 | = | 46.8 | nM | 7.33 |
| CHEMBL6024579 | — | EC50 | = | 50.3 | nM | 7.30 |
| CHEMBL5769135 | — | EC50 | = | 50.5 | nM | 7.30 |
| CHEMBL5741266 | — | EC50 | = | 54.4 | nM | 7.26 |
| CHEMBL5989702 | — | EC50 | = | 76.4 | nM | 7.12 |
| CHEMBL5860580 | — | EC50 | = | 78.8 | nM | 7.10 |
| CHEMBL6000653 | — | EC50 | = | 91.2 | nM | 7.04 |
| CHEMBL5943989 | — | EC50 | = | 95.9 | nM | 7.02 |
| CHEMBL5954441 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL5869365 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL6053005 | — | EC50 | = | 253.0 | nM | 6.60 |
| CHEMBL5963315 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL6062652 | — | EC50 | = | 349.0 | nM | 6.46 |