Assay Detail
Binding
CHEMBL4026937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of CFTR F508del mutant (unknown origin) expressed in human CFBE41o cells incubated for 10 mins in presence of forskolin measured for 7 secs by YFP halide assay
45
Total Activities
28
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 N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 7.56 | 9.27 |
| Activity | 18 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084934 | — | — | 2 | 9.27 |
| CHEMBL4087529 | — | — | 2 | 8.70 |
| CHEMBL4066158 | — | — | 2 | 8.70 |
| CHEMBL4102980 | — | — | 2 | 8.57 |
| CHEMBL4103906 | — | — | 2 | 8.52 |
| CHEMBL4075348 | — | — | 2 | 8.52 |
| CHEMBL4059736 | — | — | 2 | 8.40 |
| CHEMBL4104967 | — | — | 2 | 8.40 |
| CHEMBL4076873 | — | — | 2 | 7.96 |
| CHEMBL4079652 | — | — | 2 | 7.89 |
| CHEMBL4087115 | — | — | 2 | 7.89 |
| CHEMBL4083374 | — | — | 2 | 7.82 |
| CHEMBL4101361 | — | — | 1 | 7.80 |
| CHEMBL4077923 | — | — | 1 | 7.64 |
| CHEMBL4085032 | — | — | 1 | 7.12 |
| CHEMBL4082311 | — | — | 1 | 7.00 |
| CHEMBL2010601 | IVACAFTOR | 4.0 | 2 | 6.90 |
| CHEMBL4067101 | — | — | 1 | 6.90 |
| CHEMBL4077574 | — | — | 2 | 6.90 |
| CHEMBL4059537 | — | — | 1 | 6.87 |
| CHEMBL4066461 | — | — | 1 | 6.83 |
| CHEMBL4081673 | — | — | 1 | 6.72 |
| CHEMBL210832 | — | — | 2 | 6.49 |
| CHEMBL4076611 | — | — | 1 | 6.33 |
| CHEMBL4078274 | — | — | 2 | 6.19 |
| CHEMBL4097262 | — | — | 2 | 6.11 |
| CHEMBL4101451 | — | — | 1 | - |
| CHEMBL4079238 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4084934 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4087529 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4066158 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4102980 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4103906 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4075348 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4104967 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4059736 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4076873 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4079652 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4087115 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4083374 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4101361 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4077923 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4085032 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4082311 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4067101 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4077574 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL2010601 | IVACAFTOR | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4059537 | — | EC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4066461 | — | EC50 | = | 147.0 | nM | 6.83 |
| CHEMBL4081673 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL210832 | — | EC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4076611 | — | EC50 | = | 467.0 | nM | 6.33 |
| CHEMBL4078274 | — | EC50 | = | 652.0 | nM | 6.19 |
| CHEMBL4097262 | — | EC50 | = | 778.0 | nM | 6.11 |
| CHEMBL4101451 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4079238 | — | Activity | = | 3.0 | % | - |
| CHEMBL210832 | — | Activity | = | 71.0 | % | - |
| CHEMBL4078274 | — | Activity | = | 72.0 | % | - |
| CHEMBL4097262 | — | Activity | = | 74.0 | % | - |
| CHEMBL4087115 | — | Activity | = | 93.0 | % | - |
| CHEMBL4104967 | — | Activity | = | 98.0 | % | - |
| CHEMBL4059736 | — | Activity | = | 111.0 | % | - |
| CHEMBL4075348 | — | Activity | = | 105.0 | % | - |
| CHEMBL4076873 | — | Activity | = | 92.0 | % | - |
| CHEMBL4079652 | — | Activity | = | 81.0 | % | - |
| CHEMBL4103906 | — | Activity | = | 107.0 | % | - |
| CHEMBL4087529 | — | Activity | = | 96.0 | % | - |
| CHEMBL4066158 | — | Activity | = | 96.0 | % | - |
| CHEMBL2010601 | IVACAFTOR | Activity | = | 100.0 | % | - |
| CHEMBL4102980 | — | Activity | = | 95.0 | % | - |
| CHEMBL4084934 | — | Activity | = | 102.0 | % | - |
| CHEMBL4077574 | — | Activity | = | 95.0 | % | - |
| CHEMBL4083374 | — | Activity | = | 105.0 | % | - |