Assay Detail
Binding
CHEMBL823916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against alpha-3-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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 7.29 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130609 | — | — | 1 | 9.28 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 8.98 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.60 |
| CHEMBL57655 | — | — | 1 | 8.38 |
| CHEMBL6421 | — | — | 1 | 8.25 |
| CHEMBL341398 | — | — | 1 | 8.17 |
| CHEMBL133272 | — | — | 1 | 8.16 |
| CHEMBL133049 | — | — | 1 | 8.13 |
| CHEMBL6655 | — | — | 1 | 8.04 |
| CHEMBL415290 | Ro-151310 | — | 1 | 8.04 |
| CHEMBL336728 | — | — | 1 | 8.00 |
| CHEMBL6659 | — | — | 1 | 7.96 |
| CHEMBL133219 | — | — | 1 | 7.89 |
| CHEMBL336377 | — | — | 1 | 7.82 |
| CHEMBL59180 | — | — | 1 | 7.78 |
| CHEMBL416450 | — | — | 1 | 7.77 |
| CHEMBL58757 | — | — | 1 | 7.73 |
| CHEMBL132529 | — | — | 1 | 7.72 |
| CHEMBL58570 | — | — | 1 | 7.60 |
| CHEMBL286594 | — | — | 1 | 7.59 |
| CHEMBL58385 | — | — | 1 | 7.58 |
| CHEMBL339163 | — | — | 1 | 7.57 |
| CHEMBL52030 | — | — | 1 | 7.56 |
| CHEMBL415293 | — | — | 1 | 7.54 |
| CHEMBL7290 | — | — | 1 | 7.52 |
| CHEMBL339165 | — | — | 1 | 7.42 |
| CHEMBL6440 | — | — | 1 | 7.37 |
| CHEMBL130416 | — | — | 1 | 7.32 |
| CHEMBL6814 | — | — | 1 | 7.30 |
| CHEMBL129855 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130609 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL6597 | Ro-154513 | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL57655 | — | Ki | = | 4.14 | nM | 8.38 |
| CHEMBL6421 | — | Ki | = | 5.66 | nM | 8.25 |
| CHEMBL341398 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL133272 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL133049 | — | Ki | = | 7.42 | nM | 8.13 |
| CHEMBL6655 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL415290 | Ro-151310 | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL336728 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL6659 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL133219 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL336377 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL59180 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL416450 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL58757 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL132529 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL58570 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL286594 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL58385 | — | Ki | = | 26.1 | nM | 7.58 |
| CHEMBL339163 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL52030 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL415293 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL7290 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL339165 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL6440 | — | Ki | = | 42.5 | nM | 7.37 |
| CHEMBL130416 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL6814 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL129855 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL134175 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL336636 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL337166 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL335888 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL133112 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL133705 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL340546 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL131977 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL339172 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL59181 | — | Ki | = | 198.4 | nM | 6.70 |
| CHEMBL300840 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL335960 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL43718 | — | Ki | = | 1125.0 | nM | 5.95 |
| CHEMBL43724 | — | Ki | = | 2739.0 | nM | 5.56 |
| CHEMBL45174 | — | Ki | = | 2907.0 | nM | 5.54 |
| CHEMBL46957 | — | Ki | = | 6266.0 | nM | 5.20 |
| CHEMBL47853 | — | Ki | = | 15409.0 | nM | 4.81 |
| CHEMBL43725 | — | Ki | = | 22125.0 | nM | 4.66 |
| CHEMBL44784 | — | Ki | > | 300.0 | nM | - |
| CHEMBL445856 | — | Ki | > | 1000.0 | nM | - |