Assay Detail
Binding
CHEMBL5167322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro151788 from human recombinant alpha5beta3gamma2 GABAA receptor stably expressed in HEK293 cell membrane assessed as inhibition constant by radioligand binding assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABA<sub>A</sub> Receptor Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 7.96 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196475 | — | — | 1 | 9.31 |
| CHEMBL5202280 | — | — | 1 | 8.72 |
| CHEMBL5174560 | — | — | 1 | 8.57 |
| CHEMBL5207799 | — | — | 1 | 8.55 |
| CHEMBL5179688 | — | — | 1 | 8.49 |
| CHEMBL5179759 | — | — | 1 | 8.44 |
| CHEMBL5185502 | — | — | 1 | 8.39 |
| CHEMBL5186978 | — | — | 1 | 8.39 |
| CHEMBL3681419 | BASMISANIL | 2.0 | 1 | 8.36 |
| CHEMBL5200451 | — | — | 1 | 8.34 |
| CHEMBL5176630 | — | — | 1 | 8.34 |
| CHEMBL5181374 | — | — | 1 | 8.15 |
| CHEMBL5178153 | — | — | 1 | 8.14 |
| CHEMBL5189787 | — | — | 1 | 8.11 |
| CHEMBL5176141 | — | — | 1 | 8.10 |
| CHEMBL5189320 | — | — | 1 | 8.08 |
| CHEMBL5176939 | — | — | 1 | 8.05 |
| CHEMBL5193778 | — | — | 1 | 8.04 |
| CHEMBL5181809 | — | — | 1 | 8.00 |
| CHEMBL5197478 | — | — | 1 | 8.00 |
| CHEMBL5193523 | — | — | 1 | 7.89 |
| CHEMBL5173957 | — | — | 1 | 7.89 |
| CHEMBL5208183 | — | — | 1 | 7.89 |
| CHEMBL5182859 | — | — | 1 | 7.85 |
| CHEMBL5170797 | — | — | 1 | 7.68 |
| CHEMBL5174424 | — | — | 1 | 7.64 |
| CHEMBL5180133 | — | — | 1 | 7.64 |
| CHEMBL5184265 | — | — | 1 | 7.55 |
| CHEMBL5207798 | — | — | 1 | 7.55 |
| CHEMBL5200752 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196475 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL5202280 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5174560 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5207799 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL5179688 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL5179759 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL5185502 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL5186978 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3681419 | BASMISANIL | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL5176630 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5200451 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5181374 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5178153 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL5189787 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL5176141 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5189320 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL5176939 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5193778 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL5197478 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL5181809 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5193523 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5173957 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5208183 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5182859 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5170797 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5174424 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5180133 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5207798 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5184265 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5200752 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL5206831 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5197481 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5200620 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL5192467 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL5199140 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL5208332 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5181673 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5195083 | — | Ki | = | 55.0 | nM | 7.26 |