Assay Detail
Binding
CHEMBL682252
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Binding affinity by displacement of [3H]Ro-151788 from recombinant human gamma-aminobutyric-acid A receptor alpha3,beta3,gamma2 stably expressed in L cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | L |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.40 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294600 | — | — | 1 | 8.47 |
| CHEMBL55565 | — | — | 1 | 8.46 |
| CHEMBL264235 | — | — | 1 | 8.42 |
| CHEMBL17468 | — | — | 1 | 8.40 |
| CHEMBL56098 | — | — | 1 | 8.39 |
| CHEMBL59478 | — | — | 1 | 8.21 |
| CHEMBL59427 | — | — | 1 | 8.17 |
| CHEMBL54422 | — | — | 1 | 7.92 |
| CHEMBL59197 | — | — | 1 | 7.92 |
| CHEMBL55022 | — | — | 1 | 7.82 |
| CHEMBL54368 | — | — | 1 | 7.64 |
| CHEMBL53619 | — | — | 1 | 7.62 |
| CHEMBL56761 | — | — | 1 | 7.60 |
| CHEMBL55570 | — | — | 1 | 7.22 |
| CHEMBL291335 | — | — | 1 | 7.14 |
| CHEMBL413325 | — | — | 1 | 7.10 |
| CHEMBL301195 | — | — | 1 | 6.68 |
| CHEMBL56746 | — | — | 1 | 6.60 |
| CHEMBL299061 | — | — | 1 | 6.60 |
| CHEMBL298732 | — | — | 1 | 6.57 |
| CHEMBL58927 | — | — | 1 | 6.57 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.56 |
| CHEMBL55467 | — | — | 1 | 6.50 |
| CHEMBL54507 | — | — | 1 | 6.29 |
| CHEMBL301010 | — | — | 1 | 6.07 |
| CHEMBL291308 | — | — | 1 | - |
| CHEMBL55777 | — | — | 1 | - |
| CHEMBL55694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294600 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL55565 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL264235 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL17468 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL56098 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL59478 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL59427 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL54422 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL59197 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL55022 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL54368 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL53619 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL56761 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL55570 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL291335 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL413325 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL301195 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL56746 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL299061 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL298732 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL58927 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL55467 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL54507 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL301010 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL291308 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL55777 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL55694 | — | Ki | > | 30000.0 | nM | - |