Assay Detail
Functional
CHEMBL856036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
IC50 evaluated by measuring contraction and relaxation of guinea pig bladder strips with KCl and glibenclamide respectively
77
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Sulfonylurea receptors; K-ATP channels (CHEMBL2095152) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP potassium channel openers. Modifications on the western region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 77 | 5.44 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348203 | — | — | 1 | 6.37 |
| CHEMBL143181 | — | — | 1 | 6.33 |
| CHEMBL49035 | CROMAKALIM | 2.0 | 1 | 6.24 |
| CHEMBL143751 | — | — | 1 | 6.22 |
| CHEMBL143281 | — | — | 1 | 5.96 |
| CHEMBL141022 | — | — | 1 | 5.89 |
| CHEMBL357137 | — | — | 1 | 5.89 |
| CHEMBL139724 | — | — | 1 | 5.85 |
| CHEMBL18861 | ZD-6169 | — | 1 | 5.80 |
| CHEMBL343195 | — | — | 1 | 5.80 |
| CHEMBL143548 | — | — | 1 | 5.80 |
| CHEMBL143691 | — | — | 1 | 5.80 |
| CHEMBL140470 | — | — | 1 | 5.75 |
| CHEMBL140684 | — | — | 1 | 5.70 |
| CHEMBL143752 | — | — | 1 | 5.66 |
| CHEMBL343080 | — | — | 1 | 5.66 |
| CHEMBL143097 | — | — | 1 | 5.64 |
| CHEMBL344492 | — | — | 1 | 5.64 |
| CHEMBL143180 | — | — | 1 | 5.58 |
| CHEMBL143408 | — | — | 1 | 5.58 |
| CHEMBL358854 | — | — | 1 | 5.58 |
| CHEMBL92840 | — | — | 1 | 5.57 |
| CHEMBL143441 | — | — | 1 | 5.57 |
| CHEMBL142181 | — | — | 1 | 5.51 |
| CHEMBL143495 | — | — | 1 | 5.47 |
| CHEMBL139557 | — | — | 1 | 5.46 |
| CHEMBL344259 | — | — | 1 | 5.42 |
| CHEMBL355915 | — | — | 1 | 5.42 |
| CHEMBL70996 | — | — | 1 | 5.42 |
| CHEMBL140790 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348203 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL143181 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL49035 | CROMAKALIM | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL143751 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL143281 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL141022 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL357137 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL139724 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL18861 | ZD-6169 | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL343195 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL143548 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL143691 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL140470 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL140684 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL343080 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL143752 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL143097 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL344492 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL143180 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL143408 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL358854 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL92840 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL143441 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL142181 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL143495 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL139557 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL355915 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL70996 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL344259 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL140790 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL140694 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL359079 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL342749 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL341965 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL141615 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL141880 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL336880 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL140609 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL336923 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL424478 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL139825 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL141285 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL142328 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL140946 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL341978 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL140271 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL141414 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL140642 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL358107 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL344802 | — | IC50 | > | 30000.0 | nM | - |