Assay Detail
Binding
CHEMBL683045
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Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2
144
Total Activities
144
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
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 | 144 | 7.03 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144753 | — | — | 1 | 8.72 |
| CHEMBL3144617 | — | — | 1 | 8.69 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.42 |
| CHEMBL415293 | — | — | 1 | 8.40 |
| CHEMBL3144697 | — | — | 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 |
| CHEMBL3144610 | — | — | 1 | 8.00 |
| CHEMBL366947 | BRETAZENIL | 2.0 | 1 | 7.90 |
| CHEMBL19732 | CGS-8216 | — | 1 | 7.77 |
| CHEMBL3144615 | — | — | 1 | 7.76 |
| CHEMBL133219 | — | — | 1 | 7.66 |
| CHEMBL7290 | — | — | 1 | 7.65 |
| CHEMBL58570 | — | — | 1 | 7.64 |
| CHEMBL286594 | — | — | 1 | 7.54 |
| CHEMBL6814 | — | — | 1 | 7.51 |
| CHEMBL341398 | — | — | 1 | 7.51 |
| CHEMBL3144698 | — | — | 1 | 7.40 |
| 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 |
| CHEMBL85861 | — | — | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144753 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3144617 | — | Ki | = | 2.03 | nM | 8.69 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3144697 | — | Ki | = | 4.0 | nM | 8.40 |
| 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 |
| CHEMBL3144610 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL366947 | BRETAZENIL | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL19732 | CGS-8216 | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3144615 | — | Ki | = | 17.3 | nM | 7.76 |
| 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 |
| CHEMBL3144698 | — | Ki | = | 40.0 | nM | 7.40 |
| 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 |
| CHEMBL85861 | — | Ki | = | 74.9 | nM | 7.13 |
| CHEMBL52030 | — | Ki | = | 83.2 | nM | 7.08 |
| CHEMBL59181 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL339165 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL339163 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL17468 | — | Ki | = | 134.0 | nM | 6.87 |
| 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 |
| CHEMBL307202 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL340546 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL337166 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL133705 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL335960 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL336636 | — | 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 |