Assay Detail
Binding
CHEMBL822165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against alpha-1-beta-3-gamma-2 GABAA/BzR receptor subtype.
56
Total Activities
56
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 56 | 7.38 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.10 |
| CHEMBL130609 | — | — | 1 | 8.82 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.48 |
| CHEMBL57655 | — | — | 1 | 8.43 |
| CHEMBL131977 | — | — | 1 | 8.24 |
| CHEMBL340546 | — | — | 1 | 8.19 |
| CHEMBL133049 | — | — | 1 | 8.17 |
| CHEMBL415290 | Ro-151310 | — | 1 | 8.17 |
| CHEMBL6421 | — | — | 1 | 8.14 |
| CHEMBL133272 | — | — | 1 | 8.08 |
| CHEMBL6659 | — | — | 1 | 8.01 |
| CHEMBL132529 | — | — | 1 | 8.00 |
| CHEMBL59180 | — | — | 1 | 8.00 |
| CHEMBL416450 | — | — | 1 | 7.95 |
| CHEMBL6655 | — | — | 1 | 7.94 |
| CHEMBL7290 | — | — | 1 | 7.89 |
| CHEMBL339165 | — | — | 1 | 7.88 |
| CHEMBL58570 | — | — | 1 | 7.83 |
| CHEMBL6440 | — | — | 1 | 7.79 |
| CHEMBL341398 | — | — | 1 | 7.77 |
| CHEMBL6814 | — | — | 1 | 7.77 |
| CHEMBL415293 | — | — | 1 | 7.76 |
| CHEMBL337166 | — | — | 1 | 7.72 |
| CHEMBL58385 | — | — | 1 | 7.69 |
| CHEMBL336728 | — | — | 1 | 7.68 |
| CHEMBL133219 | — | — | 1 | 7.58 |
| CHEMBL58757 | — | — | 1 | 7.57 |
| CHEMBL286594 | — | — | 1 | 7.55 |
| CHEMBL52030 | — | — | 1 | 7.31 |
| CHEMBL336377 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL130609 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL57655 | — | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL131977 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL340546 | — | Ki | = | 6.44 | nM | 8.19 |
| CHEMBL133049 | — | Ki | = | 6.74 | nM | 8.17 |
| CHEMBL415290 | Ro-151310 | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL6421 | — | Ki | = | 7.25 | nM | 8.14 |
| CHEMBL133272 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL6659 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL132529 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL59180 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL416450 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL6655 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL7290 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL339165 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL58570 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL6440 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL341398 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL6814 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL415293 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL337166 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL58385 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL336728 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL133219 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL58757 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL286594 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL52030 | — | Ki | = | 48.5 | nM | 7.31 |
| CHEMBL336377 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL339163 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL335888 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL130416 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL134175 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL336636 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL59181 | — | Ki | = | 121.1 | nM | 6.92 |
| CHEMBL133705 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL300840 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL129855 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL339172 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL335960 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL133112 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL43718 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL43724 | — | Ki | = | 1581.0 | nM | 5.80 |
| CHEMBL45174 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL46957 | — | Ki | = | 4201.0 | nM | 5.38 |
| CHEMBL47853 | — | Ki | = | 9483.0 | nM | 5.02 |
| CHEMBL43725 | — | Ki | = | 17535.0 | nM | 4.76 |
| CHEMBL45346 | — | Ki | > | 300.0 | nM | - |
| CHEMBL445856 | — | Ki | > | 1000.0 | nM | - |