Assay Detail
Binding
CHEMBL898326
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Displacement of [3H]EBOB from human recombinant GABAbeta3 receptor expressed in HEK293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Gamma-aminobutyric acid receptor subunit beta-3 (CHEMBL1847) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, 3D-QSAR, and docking studies of 1-phenyl-1H-1,2,3-triazoles as selective antagonists for beta3 over alpha1beta2gamma2 GABA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.63 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235623 | — | — | 1 | 9.18 |
| CHEMBL236471 | — | — | 1 | 8.71 |
| CHEMBL395136 | — | — | 1 | 8.60 |
| CHEMBL392036 | — | — | 1 | 8.37 |
| CHEMBL392035 | — | — | 1 | 8.15 |
| CHEMBL236671 | — | — | 1 | 8.09 |
| CHEMBL396305 | — | — | 1 | 7.87 |
| CHEMBL235405 | — | — | 1 | 7.33 |
| CHEMBL395137 | — | — | 1 | 7.18 |
| CHEMBL236470 | — | — | 1 | 7.15 |
| CHEMBL235406 | — | — | 1 | 6.89 |
| CHEMBL428023 | — | — | 1 | 6.27 |
| CHEMBL235407 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235623 | — | Ki | = | 0.659 | nM | 9.18 |
| CHEMBL236471 | — | Ki | = | 1.94 | nM | 8.71 |
| CHEMBL395136 | — | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL392036 | — | Ki | = | 4.27 | nM | 8.37 |
| CHEMBL392035 | — | Ki | = | 7.08 | nM | 8.15 |
| CHEMBL236671 | — | Ki | = | 8.07 | nM | 8.09 |
| CHEMBL396305 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL235405 | — | Ki | = | 47.2 | nM | 7.33 |
| CHEMBL395137 | — | Ki | = | 66.7 | nM | 7.18 |
| CHEMBL236470 | — | Ki | = | 70.1 | nM | 7.15 |
| CHEMBL235406 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL428023 | — | Ki | = | 539.0 | nM | 6.27 |
| CHEMBL235407 | — | Ki | = | 3450.0 | nM | 5.46 |