Assay Detail
Binding
CHEMBL1817224
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Binding affinity to CFTR F508 deletion mutant expressed in forskolin-stimulated FRT cells assessed as increase in iodine influx measured as YFP quenching rate after 24 hrs by fluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | FRT |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Cystic fibrosis: a new target for 4-Imidazo[2,1-b]thiazole-1,4-dihydropyridines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 23 | 5.41 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1814700 | — | — | 1 | 6.77 |
| CHEMBL1814576 | — | — | 1 | 6.75 |
| CHEMBL1814577 | — | — | 1 | 6.50 |
| CHEMBL1814699 | — | — | 1 | 6.43 |
| CHEMBL1814701 | — | — | 1 | 6.40 |
| CHEMBL272211 | — | — | 1 | 5.85 |
| CHEMBL411450 | — | — | 1 | 5.55 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 5.54 |
| CHEMBL1814575 | — | — | 1 | 5.50 |
| CHEMBL1814584 | — | — | 1 | 5.50 |
| CHEMBL1814578 | — | — | 1 | 5.46 |
| CHEMBL1814579 | — | — | 1 | 5.32 |
| CHEMBL271969 | — | — | 1 | 5.17 |
| CHEMBL1814583 | — | — | 1 | 5.08 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.03 |
| CHEMBL410241 | — | — | 1 | 4.96 |
| CHEMBL272810 | — | — | 1 | 4.92 |
| CHEMBL1814580 | — | — | 1 | 4.83 |
| CHEMBL1814574 | — | — | 1 | 4.71 |
| CHEMBL270674 | — | — | 1 | 4.67 |
| CHEMBL272472 | — | — | 1 | 4.55 |
| CHEMBL411235 | — | — | 1 | 4.47 |
| CHEMBL271970 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1814700 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL1814576 | — | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1814577 | — | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL1814699 | — | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL1814701 | — | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL272211 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL411450 | — | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL193 | NIFEDIPINE | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL1814575 | — | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL1814584 | — | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL1814578 | — | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL1814579 | — | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL271969 | — | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL1814583 | — | Kd | = | 8400.0 | nM | 5.08 |
| CHEMBL44 | GENISTEIN | Kd | = | 9400.0 | nM | 5.03 |
| CHEMBL410241 | — | Kd | = | 10900.0 | nM | 4.96 |
| CHEMBL272810 | — | Kd | = | 12000.0 | nM | 4.92 |
| CHEMBL1814580 | — | Kd | = | 14800.0 | nM | 4.83 |
| CHEMBL1814574 | — | Kd | = | 19400.0 | nM | 4.71 |
| CHEMBL270674 | — | Kd | = | 21400.0 | nM | 4.67 |
| CHEMBL272472 | — | Kd | = | 28300.0 | nM | 4.55 |
| CHEMBL411235 | — | Kd | = | 34200.0 | nM | 4.47 |
| CHEMBL271970 | — | Kd | = | 42900.0 | nM | 4.37 |