Assay Detail
Binding
CHEMBL3706142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Competition Binding Assay: The affinity of the test compounds was determined by radioligand competition binding assay, using the known compound [3H]Ro-15-1788 (Flumazenil) (Perkin Elmer, 85.4 Ci/mmol) and the human recombinant GABA A receptor containing the alpha2, beta2, and gamma3 subunits.Membranes were prepared from HEK cells expressing hGABA A alpha2beta2- gamma3 receptor, and validated to ascertain protein concentration, receptor expression and to determine the Kd of the flumazenil as well as the Ki of a standard set of compounds before being used to test new compounds.The assay was carried out in 96 well plates; testing compounds using a 10 point semi-log dilution range from 19 uM top concentration. 100 ul of radioligand and 100 ul of membrane in 50 mM Tris-HCI and 0.05% F127 with 1 ul of test compound was incubated for 2 hours to allow the reaction to achieve equilibrium, and then harvested onto filter plates, dried and counted on a TopCount NXT. The data was analysed, and the Ki values were presented.
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-2 (CHEMBL4956) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Chemical compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 50 | 7.41 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647535 | — | — | 1 | 8.29 |
| CHEMBL3647548 | — | — | 1 | 8.23 |
| CHEMBL3647561 | — | — | 1 | 8.13 |
| CHEMBL3647565 | — | — | 1 | 8.13 |
| CHEMBL3647579 | — | — | 1 | 8.07 |
| CHEMBL3647538 | — | — | 1 | 8.02 |
| CHEMBL3647539 | — | — | 1 | 8.01 |
| CHEMBL3647534 | — | — | 1 | 7.96 |
| CHEMBL3647566 | — | — | 1 | 7.93 |
| CHEMBL3647581 | — | — | 1 | 7.85 |
| CHEMBL3647580 | — | — | 1 | 7.84 |
| CHEMBL3647549 | — | — | 1 | 7.79 |
| CHEMBL3647562 | — | — | 1 | 7.75 |
| CHEMBL3647568 | — | — | 1 | 7.74 |
| CHEMBL3647578 | — | — | 1 | 7.72 |
| CHEMBL3647571 | — | — | 1 | 7.72 |
| CHEMBL3647559 | — | — | 1 | 7.66 |
| CHEMBL3647547 | — | — | 1 | 7.62 |
| CHEMBL3647582 | — | — | 1 | 7.54 |
| CHEMBL3647555 | — | — | 1 | 7.53 |
| CHEMBL3647541 | — | — | 1 | 7.51 |
| CHEMBL3647533 | — | — | 1 | 7.51 |
| CHEMBL3647543 | — | — | 1 | 7.46 |
| CHEMBL3647550 | — | — | 1 | 7.46 |
| CHEMBL3647567 | — | — | 1 | 7.45 |
| CHEMBL3647575 | — | — | 1 | 7.43 |
| CHEMBL3647564 | — | — | 1 | 7.41 |
| CHEMBL3647551 | — | — | 1 | 7.41 |
| CHEMBL3647574 | — | — | 1 | 7.39 |
| CHEMBL3647557 | — | — | 1 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647535 | — | Ki | = | 5.08 | nM | 8.29 |
| CHEMBL3647548 | — | Ki | = | 5.82 | nM | 8.23 |
| CHEMBL3647565 | — | Ki | = | 7.48 | nM | 8.13 |
| CHEMBL3647561 | — | Ki | = | 7.45 | nM | 8.13 |
| CHEMBL3647579 | — | Ki | = | 8.56 | nM | 8.07 |
| CHEMBL3647538 | — | Ki | = | 9.51 | nM | 8.02 |
| CHEMBL3647539 | — | Ki | = | 9.71 | nM | 8.01 |
| CHEMBL3647534 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL3647566 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL3647581 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3647580 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL3647549 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL3647562 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL3647568 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL3647571 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3647578 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL3647559 | — | Ki | = | 21.7 | nM | 7.66 |
| CHEMBL3647547 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL3647582 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL3647555 | — | Ki | = | 29.7 | nM | 7.53 |
| CHEMBL3647541 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL3647533 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL3647543 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL3647550 | — | Ki | = | 34.5 | nM | 7.46 |
| CHEMBL3647567 | — | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL3647575 | — | Ki | = | 37.1 | nM | 7.43 |
| CHEMBL3647551 | — | Ki | = | 38.8 | nM | 7.41 |
| CHEMBL3647564 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL3647574 | — | Ki | = | 40.5 | nM | 7.39 |
| CHEMBL3647557 | — | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL3647572 | — | Ki | = | 43.3 | nM | 7.36 |
| CHEMBL3647569 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3647563 | — | Ki | = | 61.3 | nM | 7.21 |
| CHEMBL3647573 | — | Ki | = | 67.8 | nM | 7.17 |
| CHEMBL3647560 | — | Ki | = | 69.5 | nM | 7.16 |
| CHEMBL3647544 | — | Ki | = | 74.3 | nM | 7.13 |
| CHEMBL3647577 | — | Ki | = | 87.4 | nM | 7.06 |
| CHEMBL3647558 | — | Ki | = | 92.2 | nM | 7.04 |
| CHEMBL3647552 | — | Ki | = | 91.4 | nM | 7.04 |
| CHEMBL3647545 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL3647570 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL3647537 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3647553 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL3647546 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3647542 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL3647576 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL3647540 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL3647554 | — | Ki | = | 678.0 | nM | 6.17 |
| CHEMBL3647556 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL3647536 | DARIGABAT | Ki | < | 2.47 | nM | - |