Assay Detail
Binding
CHEMBL685338
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Binding affinity for Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2
58
Total Activities
58
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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 58 | 8.31 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130609 | — | — | 1 | 9.85 |
| CHEMBL6597 | Ro-154513 | — | 1 | 9.57 |
| CHEMBL133049 | — | — | 1 | 9.53 |
| CHEMBL6421 | — | — | 1 | 9.52 |
| CHEMBL341398 | — | — | 1 | 9.52 |
| CHEMBL336728 | — | — | 1 | 9.43 |
| CHEMBL6659 | — | — | 1 | 9.42 |
| CHEMBL58757 | — | — | 1 | 9.40 |
| CHEMBL133272 | — | — | 1 | 9.40 |
| CHEMBL52030 | — | — | 1 | 9.35 |
| CHEMBL6655 | — | — | 1 | 9.33 |
| CHEMBL286594 | — | — | 1 | 9.31 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.22 |
| CHEMBL415293 | — | — | 1 | 9.19 |
| CHEMBL133219 | — | — | 1 | 9.15 |
| CHEMBL339165 | — | — | 1 | 9.11 |
| CHEMBL415290 | Ro-151310 | — | 1 | 9.07 |
| CHEMBL336377 | — | — | 1 | 9.00 |
| CHEMBL416450 | — | — | 1 | 8.97 |
| CHEMBL57655 | — | — | 1 | 8.96 |
| CHEMBL339163 | — | — | 1 | 8.89 |
| CHEMBL58385 | — | — | 1 | 8.82 |
| CHEMBL59180 | — | — | 1 | 8.78 |
| CHEMBL58570 | — | — | 1 | 8.76 |
| CHEMBL134175 | — | — | 1 | 8.62 |
| CHEMBL6814 | — | — | 1 | 8.60 |
| CHEMBL130416 | — | — | 1 | 8.59 |
| CHEMBL300840 | — | — | 1 | 8.58 |
| CHEMBL7290 | — | — | 1 | 8.46 |
| CHEMBL336636 | — | — | 1 | 8.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130609 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL6597 | Ro-154513 | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL133049 | — | Ki | = | 0.293 | nM | 9.53 |
| CHEMBL6421 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL341398 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL336728 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL6659 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL58757 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL133272 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL52030 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL6655 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL286594 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL415293 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL133219 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL339165 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL415290 | Ro-151310 | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL336377 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL416450 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL57655 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL339163 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL58385 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL59180 | — | Ki | = | 1.68 | nM | 8.78 |
| CHEMBL58570 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL134175 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL6814 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL130416 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL300840 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL7290 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL336636 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL129855 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL340546 | — | Ki | = | 4.23 | nM | 8.37 |
| CHEMBL335888 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL59181 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL132529 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL133112 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL337166 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL133705 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL131977 | — | Ki | = | 9.25 | nM | 8.03 |
| CHEMBL6440 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL339172 | — | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL335960 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL44784 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL45346 | — | Ki | = | 38.8 | nM | 7.41 |
| CHEMBL295981 | — | Ki | = | 82.7 | nM | 7.08 |
| CHEMBL445856 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL43724 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL43718 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL45174 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL133914 | — | Ki | = | 374.0 | nM | 6.43 |