Assay Detail
Binding
CHEMBL678329
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Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2
146
Total Activities
146
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 146 | 7.82 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | — | 1 | 10.30 |
| CHEMBL3144697 | — | — | 1 | 10.22 |
| CHEMBL3144849 | — | — | 1 | 10.15 |
| CHEMBL3144696 | — | — | 1 | 10.10 |
| CHEMBL3144841 | — | — | 1 | 9.96 |
| CHEMBL10483 | — | — | 1 | 9.85 |
| CHEMBL3144698 | — | — | 1 | 9.74 |
| CHEMBL3144753 | — | — | 1 | 9.70 |
| CHEMBL3144615 | — | — | 1 | 9.64 |
| CHEMBL3144610 | — | — | 1 | 9.47 |
| CHEMBL366947 | BRETAZENIL | 2.0 | 1 | 9.46 |
| CHEMBL307202 | — | — | 1 | 9.40 |
| CHEMBL170808 | — | — | 1 | 9.31 |
| CHEMBL49141 | — | — | 1 | 9.31 |
| CHEMBL10534 | — | — | 1 | 9.20 |
| CHEMBL307783 | — | — | 1 | 9.14 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 9.10 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.10 |
| CHEMBL301605 | — | — | 1 | 8.96 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.92 |
| CHEMBL11709 | — | — | 1 | 8.92 |
| CHEMBL3144617 | — | — | 1 | 8.87 |
| CHEMBL130609 | — | — | 1 | 8.82 |
| CHEMBL173329 | — | — | 1 | 8.80 |
| CHEMBL10195 | — | — | 1 | 8.70 |
| CHEMBL69719 | — | — | 1 | 8.68 |
| CHEMBL173193 | — | — | 1 | 8.66 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.66 |
| CHEMBL177076 | — | — | 1 | 8.62 |
| CHEMBL173938 | — | — | 1 | 8.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL3144697 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL3144849 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL3144696 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3144841 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL10483 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL3144698 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL3144753 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3144615 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3144610 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL366947 | BRETAZENIL | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL307202 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL49141 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL170808 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL10534 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL307783 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL646 | TRIAZOLAM | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL301605 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL267665 | RO-147437 | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL11709 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3144617 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL130609 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL173329 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL10195 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL69719 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL173193 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL177076 | — | Ki | = | 2.39 | nM | 8.62 |
| CHEMBL3144795 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL173938 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL173219 | — | Ki | = | 3.41 | nM | 8.47 |
| CHEMBL141039 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL57655 | — | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL439945 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1518572 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL79945 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL52750 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL268262 | — | Ki | = | 5.42 | nM | 8.27 |
| CHEMBL17468 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL131977 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL85861 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL299250 | — | Ki | = | 6.43 | nM | 8.19 |
| CHEMBL340546 | — | Ki | = | 6.44 | nM | 8.19 |
| CHEMBL415290 | Ro-151310 | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL133049 | — | Ki | = | 6.74 | nM | 8.17 |
| CHEMBL6421 | — | Ki | = | 7.25 | nM | 8.14 |
| CHEMBL10597 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL173082 | — | Ki | = | 7.3 | nM | 8.14 |