Assay Detail
Binding
CHEMBL683047
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Binding affinity against Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-6/beta-3/gamma-2 (CHEMBL2095190) ↗| 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 | 55 | 6.98 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 8.42 |
| CHEMBL415293 | — | — | 1 | 8.40 |
| CHEMBL6659 | — | — | 1 | 8.34 |
| CHEMBL58757 | — | — | 1 | 8.29 |
| CHEMBL6421 | — | — | 1 | 8.28 |
| CHEMBL130609 | — | — | 1 | 8.16 |
| CHEMBL133049 | — | — | 1 | 8.08 |
| CHEMBL6655 | — | — | 1 | 8.03 |
| CHEMBL133219 | — | — | 1 | 7.66 |
| CHEMBL7290 | — | — | 1 | 7.65 |
| CHEMBL58570 | — | — | 1 | 7.64 |
| CHEMBL286594 | — | — | 1 | 7.54 |
| CHEMBL341398 | — | — | 1 | 7.51 |
| CHEMBL6814 | — | — | 1 | 7.51 |
| CHEMBL336728 | — | — | 1 | 7.38 |
| CHEMBL57655 | — | — | 1 | 7.35 |
| CHEMBL336377 | — | — | 1 | 7.34 |
| CHEMBL416450 | — | — | 1 | 7.29 |
| CHEMBL415290 | Ro-151310 | — | 1 | 7.26 |
| CHEMBL300840 | — | — | 1 | 7.23 |
| CHEMBL133112 | — | — | 1 | 7.21 |
| CHEMBL52030 | — | — | 1 | 7.08 |
| CHEMBL59181 | — | — | 1 | 6.94 |
| CHEMBL339165 | — | — | 1 | 6.93 |
| CHEMBL339163 | — | — | 1 | 6.90 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 6.83 |
| CHEMBL134175 | — | — | 1 | 6.82 |
| CHEMBL6440 | — | — | 1 | 6.78 |
| CHEMBL58385 | — | — | 1 | 6.75 |
| CHEMBL130416 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL415293 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL6659 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL58757 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL6421 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL130609 | — | Ki | = | 6.89 | nM | 8.16 |
| CHEMBL133049 | — | Ki | = | 8.28 | nM | 8.08 |
| CHEMBL6655 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL133219 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL7290 | — | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL58570 | — | Ki | = | 22.9 | nM | 7.64 |
| CHEMBL286594 | — | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL341398 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL6814 | — | Ki | = | 30.7 | nM | 7.51 |
| CHEMBL336728 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL57655 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL336377 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL416450 | — | Ki | = | 51.5 | nM | 7.29 |
| CHEMBL415290 | Ro-151310 | Ki | = | 54.6 | nM | 7.26 |
| CHEMBL300840 | — | Ki | = | 58.6 | nM | 7.23 |
| CHEMBL133112 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL52030 | — | Ki | = | 83.2 | nM | 7.08 |
| CHEMBL59181 | — | Ki | = | 113.7 | nM | 6.94 |
| CHEMBL339165 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL339163 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL134175 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL6440 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL58385 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL130416 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL340546 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL337166 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL133705 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL336636 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL335960 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL131977 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL335888 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL129855 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL339172 | — | Ki | = | 361.0 | nM | 6.44 |
| CHEMBL45174 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL43724 | — | Ki | = | 2930.0 | nM | 5.53 |
| CHEMBL43718 | — | Ki | = | 3648.0 | nM | 5.44 |
| CHEMBL46957 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL43725 | — | Ki | = | 29500.0 | nM | 4.53 |
| CHEMBL47853 | — | Ki | = | 30160.0 | nM | 4.52 |
| CHEMBL336133 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL59180 | — | Ki | > | 100.0 | nM | - |
| CHEMBL445856 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL295981 | — | Ki | > | 300.0 | nM | - |
| CHEMBL432104 | — | Ki | > | 300.0 | nM | - |