Assay Detail
Binding
CHEMBL991887
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor
31
Total Activities
31
Compounds Tested
2
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-5 (CHEMBL5112) ↗| 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 | 7.87 | 9.30 |
| Ki | 10 | 7.24 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.30 |
| CHEMBL458147 | — | — | 1 | 9.19 |
| CHEMBL415290 | Ro-151310 | — | 1 | 9.07 |
| CHEMBL85861 | — | — | 1 | 9.00 |
| CHEMBL454865 | — | — | 1 | 8.82 |
| CHEMBL130416 | — | — | 1 | 8.59 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.52 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.42 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 8.40 |
| CHEMBL518197 | — | — | 1 | 8.40 |
| CHEMBL461716 | — | — | 1 | 8.30 |
| CHEMBL3144739 | — | — | 1 | 8.30 |
| CHEMBL174535 | — | — | 1 | 8.15 |
| CHEMBL454095 | ABECARNIL | 2.0 | 1 | 8.08 |
| CHEMBL458319 | — | — | 1 | 8.01 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.64 |
| CHEMBL11709 | — | — | 1 | 7.57 |
| CHEMBL20042 | CGS-9896 | — | 1 | 7.40 |
| CHEMBL453066 | BETA-CCM | — | 1 | 7.24 |
| CHEMBL461717 | — | — | 1 | 7.24 |
| CHEMBL459031 | — | — | 1 | 7.08 |
| CHEMBL307783 | — | — | 1 | 6.96 |
| CHEMBL511685 | — | — | 1 | 6.78 |
| CHEMBL458321 | — | — | 1 | 6.74 |
| CHEMBL19732 | CGS-8216 | — | 1 | 6.70 |
| CHEMBL471115 | — | — | 1 | 6.43 |
| CHEMBL461511 | — | — | 1 | 6.30 |
| CHEMBL52750 | — | — | 1 | 6.23 |
| CHEMBL299250 | — | — | 1 | 6.08 |
| CHEMBL458320 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL458147 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL415290 | Ro-151310 | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL85861 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL454865 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL130416 | — | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL13280 | FLUNITRAZEPAM | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL6597 | Ro-154513 | Kd | = | 3.8 | nM | 8.42 |
| CHEMBL646 | TRIAZOLAM | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL518197 | — | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL461716 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL3144739 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL174535 | — | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL454095 | ABECARNIL | Kd | = | 8.4 | nM | 8.08 |
| CHEMBL458319 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL12 | DIAZEPAM | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL11709 | — | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL20042 | CGS-9896 | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL453066 | BETA-CCM | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL461717 | — | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL459031 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL307783 | — | Kd | = | 111.0 | nM | 6.96 |
| CHEMBL511685 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL458321 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL19732 | CGS-8216 | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL471115 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL461511 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL52750 | — | Kd | = | 591.0 | nM | 6.23 |
| CHEMBL299250 | — | Kd | = | 826.0 | nM | 6.08 |
| CHEMBL458320 | — | Ki | = | 2610.0 | nM | 5.58 |
| CHEMBL510963 | — | Ki | > | 300.0 | nM | - |