Assay Detail
ADMET
CHEMBL4351507
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-flumazenil from human GABAA alpha1beta3gamma2 receptor expressed in HEK293 cell membranes measured after 2 hrs by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design and Identification of a Novel, Functionally Subtype Selective GABA<sub>A</sub> Positive Allosteric Modulator (PF-06372865).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 9.47 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647536 | DARIGABAT | 2.0 | 1 | 9.74 |
| CHEMBL4545044 | — | — | 1 | 9.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647536 | DARIGABAT | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4545044 | — | Ki | = | 0.64 | nM | 9.19 |