Assay Detail
Binding
CHEMBL5735700
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition In Vito Assay: The investigations on the inhibition of the recombinant TASK-1 and TASK-3 channels were carried out using stably transfected CHO cells. Here, the compounds according to the invention were tested with administration of 40 mM of potassium chloride in the presence of a voltage-sensitive dye for high-throughput screening of potassium channel from Molecular Devices FLIPR Application Note: Measuring membrane potential using the FLIPR membrane potential assay kit on Fluorometric Imaging Plate Reader (FLIPR) systems. The activity of the test substances was determined as their ability to inhibit a depolarization induced in the recombinant cells by 40 mM potassium chloride.
258
Total Activities
77
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Potassium channel subfamily K member 3 (CHEMBL2321613) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-phenyl-3-(piperazinomethyl)imidazo[1,2-A]pyridine derivatives as blockers of task-1 and task-2 channels, for the treatment of sleep-related breathing disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 86 | 6.33 | 8.55 |
| kon | 86 | - | - |
| k_off | 86 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5883778 | — | — | 6 | 8.55 |
| CHEMBL5976530 | — | — | 6 | 8.38 |
| CHEMBL5953514 | — | — | 6 | 8.37 |
| CHEMBL5979320 | — | — | 6 | 8.31 |
| CHEMBL6016320 | — | — | 6 | 8.10 |
| CHEMBL5189300 | — | — | 6 | 8.01 |
| CHEMBL5781241 | — | — | 6 | 7.87 |
| CHEMBL5172358 | — | — | 3 | 7.38 |
| CHEMBL5932536 | — | — | 6 | 7.35 |
| CHEMBL5955132 | — | — | 3 | 7.18 |
| CHEMBL5928540 | — | — | 3 | 7.17 |
| CHEMBL5948731 | — | — | 3 | 7.15 |
| CHEMBL6050684 | — | — | 3 | 7.03 |
| CHEMBL5922163 | — | — | 3 | 6.77 |
| CHEMBL5932576 | — | — | 3 | 6.66 |
| CHEMBL5955974 | — | — | 3 | 6.64 |
| CHEMBL5937118 | — | — | 3 | 6.63 |
| CHEMBL6013481 | — | — | 3 | 6.62 |
| CHEMBL5833962 | — | — | 3 | 6.57 |
| CHEMBL5877257 | — | — | 3 | 6.52 |
| CHEMBL5870683 | — | — | 3 | 6.52 |
| CHEMBL5936147 | — | — | 3 | 6.51 |
| CHEMBL5742220 | — | — | 3 | 6.46 |
| CHEMBL5756587 | — | — | 3 | 6.43 |
| CHEMBL5870080 | — | — | 3 | 6.42 |
| CHEMBL5822460 | — | — | 3 | 6.41 |
| CHEMBL5918386 | — | — | 3 | 6.40 |
| CHEMBL6028256 | — | — | 3 | 6.39 |
| CHEMBL5995367 | — | — | 3 | 6.37 |
| CHEMBL5885901 | — | — | 3 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5883778 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5976530 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5953514 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5979320 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL6016320 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5189300 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5781241 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL5172358 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5932536 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5883778 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5955132 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5928540 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5948731 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL6016320 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL6050684 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5976530 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL5979320 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5922163 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5189300 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5932576 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5955974 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5937118 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL6013481 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL5833962 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5870683 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL5877257 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL5936147 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5742220 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5756587 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5870080 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL5822460 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL5918386 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL6028256 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL5995367 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5781241 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5885901 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL5953514 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL6001517 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL5932536 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5748467 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5881187 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5794705 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL6049147 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL5767153 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL6007773 | — | IC50 | = | 551.0 | nM | 6.26 |
| CHEMBL6058665 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5867797 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL5816701 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL5763659 | — | IC50 | = | 685.0 | nM | 6.16 |
| CHEMBL6005294 | — | IC50 | = | 708.0 | nM | 6.15 |