Assay Detail
Binding
CHEMBL678746
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity for human GABA-A receptor alpha-5-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 | 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
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 | 8.90 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 9.52 |
| CHEMBL58757 | — | — | 1 | 9.40 |
| CHEMBL52030 | — | — | 1 | 9.35 |
| CHEMBL286594 | — | — | 1 | 9.31 |
| CHEMBL300840 | — | — | 1 | 8.58 |
| CHEMBL59181 | — | — | 1 | 8.30 |
| CHEMBL35571 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL58757 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL52030 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL286594 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL300840 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL59181 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL35571 | — | Ki | = | 15.0 | nM | 7.82 |