Assay Detail
Binding
CHEMBL873179
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In vitro binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits expressed in L(tk-) cell membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.13 | 7.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58757 | — | — | 1 | 7.73 |
| CHEMBL52030 | — | — | 1 | 7.61 |
| CHEMBL6597 | Ro-154513 | — | 1 | 7.60 |
| CHEMBL286594 | — | — | 1 | 7.59 |
| CHEMBL59181 | — | — | 1 | 6.70 |
| CHEMBL300840 | — | — | 1 | 6.59 |
| CHEMBL35571 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58757 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL52030 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL6597 | Ro-154513 | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL286594 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL59181 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL300840 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL35571 | — | Ki | = | 858.0 | nM | 6.07 |