Assay Detail
Binding
CHEMBL991886
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-1 (CHEMBL1962) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 8.24 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144739 | — | — | 1 | 10.00 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.52 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 9.00 |
| CHEMBL454095 | ABECARNIL | 2.0 | 1 | 9.00 |
| CHEMBL11709 | — | — | 1 | 9.00 |
| CHEMBL307783 | — | — | 1 | 9.00 |
| CHEMBL453066 | BETA-CCM | — | 1 | 9.00 |
| CHEMBL299250 | — | — | 1 | 8.92 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 8.70 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.48 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.35 |
| CHEMBL52750 | — | — | 1 | 8.30 |
| CHEMBL85861 | — | — | 1 | 8.10 |
| CHEMBL19732 | CGS-8216 | — | 1 | 8.08 |
| CHEMBL454865 | — | — | 1 | 7.69 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.44 |
| CHEMBL174535 | — | — | 1 | 7.12 |
| CHEMBL130416 | — | — | 1 | 7.08 |
| CHEMBL461716 | — | — | 1 | 6.92 |
| CHEMBL461717 | — | — | 1 | 6.71 |
| CHEMBL518197 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144739 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL20042 | CGS-9896 | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL646 | TRIAZOLAM | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL454095 | ABECARNIL | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL11709 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL307783 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL453066 | BETA-CCM | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL299250 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL407 | FLUMAZENIL | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL6597 | Ro-154513 | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL13280 | FLUNITRAZEPAM | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL52750 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL85861 | — | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL19732 | CGS-8216 | Kd | = | 8.3 | nM | 8.08 |
| CHEMBL454865 | — | Kd | = | 20.4 | nM | 7.69 |
| CHEMBL12 | DIAZEPAM | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL174535 | — | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL130416 | — | Kd | = | 83.0 | nM | 7.08 |
| CHEMBL461716 | — | Kd | = | 121.0 | nM | 6.92 |
| CHEMBL461717 | — | Kd | = | 197.0 | nM | 6.71 |
| CHEMBL518197 | — | Kd | = | 200.0 | nM | 6.70 |