Assay Detail
Binding
CHEMBL824296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity tested against alpha-2-beta-3-gamma-2 GABAA/BzR receptor subtype.
49
Total Activities
49
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| 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 | 49 | 7.13 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.05 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.59 |
| CHEMBL57655 | — | — | 1 | 8.14 |
| CHEMBL133272 | — | — | 1 | 7.99 |
| CHEMBL6655 | — | — | 1 | 7.97 |
| CHEMBL6659 | — | — | 1 | 7.95 |
| CHEMBL336728 | — | — | 1 | 7.92 |
| CHEMBL341398 | — | — | 1 | 7.89 |
| CHEMBL415290 | Ro-151310 | — | 1 | 7.79 |
| CHEMBL415293 | — | — | 1 | 7.67 |
| CHEMBL286594 | — | — | 1 | 7.67 |
| CHEMBL59180 | — | — | 1 | 7.65 |
| CHEMBL58757 | — | — | 1 | 7.58 |
| CHEMBL58385 | — | — | 1 | 7.57 |
| CHEMBL52030 | — | — | 1 | 7.56 |
| CHEMBL336377 | — | — | 1 | 7.54 |
| CHEMBL6814 | — | — | 1 | 7.47 |
| CHEMBL416450 | — | — | 1 | 7.44 |
| CHEMBL134175 | — | — | 1 | 7.40 |
| CHEMBL339163 | — | — | 1 | 7.36 |
| CHEMBL132529 | — | — | 1 | 7.35 |
| CHEMBL6440 | — | — | 1 | 7.32 |
| CHEMBL7290 | — | — | 1 | 7.30 |
| CHEMBL58570 | — | — | 1 | 7.25 |
| CHEMBL337166 | — | — | 1 | 7.25 |
| CHEMBL130416 | — | — | 1 | 7.22 |
| CHEMBL336636 | — | — | 1 | 7.16 |
| CHEMBL335888 | — | — | 1 | 7.07 |
| CHEMBL133705 | — | — | 1 | 7.06 |
| CHEMBL129855 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL6597 | Ro-154513 | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL57655 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL133272 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL6655 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL6659 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL336728 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL341398 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL415290 | Ro-151310 | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL415293 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL286594 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL59180 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL58757 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL58385 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL52030 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL336377 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL6814 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL416450 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL134175 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL339163 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL132529 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL6440 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL7290 | — | Ki | = | 49.8 | nM | 7.30 |
| CHEMBL337166 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL58570 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL130416 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL336636 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL335888 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL133705 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL129855 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL59181 | — | Ki | = | 141.9 | nM | 6.85 |
| CHEMBL300840 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL339172 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL133112 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL335960 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL43718 | — | Ki | = | 1527.0 | nM | 5.82 |
| CHEMBL45174 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL43724 | — | Ki | = | 2865.0 | nM | 5.54 |
| CHEMBL46957 | — | Ki | = | 12590.0 | nM | 4.90 |
| CHEMBL47853 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL43725 | — | Ki | = | 33834.0 | nM | 4.47 |
| CHEMBL336133 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL432104 | — | Ki | > | 300.0 | nM | - |
| CHEMBL45346 | — | Ki | > | 300.0 | nM | - |
| CHEMBL44784 | — | Ki | > | 300.0 | nM | - |
| CHEMBL445856 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL295277 | — | Ki | > | 300.0 | nM | - |
| CHEMBL134241 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL295981 | — | Ki | > | 300.0 | nM | - |