Assay Detail
Binding
CHEMBL681248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2
136
Total Activities
136
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| 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 | 136 | 7.50 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144849 | — | — | 1 | 10.52 |
| CHEMBL3144696 | — | — | 1 | 10.22 |
| CHEMBL19732 | CGS-8216 | — | 1 | 10.10 |
| CHEMBL3144697 | — | — | 1 | 10.10 |
| CHEMBL3144841 | — | — | 1 | 10.00 |
| CHEMBL3144615 | — | — | 1 | 9.77 |
| CHEMBL3144698 | — | — | 1 | 9.68 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 9.23 |
| CHEMBL366947 | BRETAZENIL | 2.0 | 1 | 9.19 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.05 |
| CHEMBL301605 | — | — | 1 | 8.92 |
| CHEMBL10483 | — | — | 1 | 8.92 |
| CHEMBL49141 | — | — | 1 | 8.92 |
| CHEMBL3144617 | — | — | 1 | 8.88 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.70 |
| CHEMBL307202 | — | — | 1 | 8.68 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.60 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.59 |
| CHEMBL10534 | — | — | 1 | 8.55 |
| CHEMBL173329 | — | — | 1 | 8.54 |
| CHEMBL3144795 | — | — | 1 | 8.43 |
| CHEMBL1518572 | — | — | 1 | 8.38 |
| CHEMBL11709 | — | — | 1 | 8.31 |
| CHEMBL10195 | — | — | 1 | 8.27 |
| CHEMBL57655 | — | — | 1 | 8.14 |
| CHEMBL17468 | — | — | 1 | 8.08 |
| CHEMBL368768 | — | — | 1 | 8.03 |
| CHEMBL133272 | — | — | 1 | 7.99 |
| CHEMBL79945 | — | — | 1 | 7.98 |
| CHEMBL6655 | — | — | 1 | 7.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144849 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3144696 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL19732 | CGS-8216 | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3144697 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3144841 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3144615 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL3144698 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL646 | TRIAZOLAM | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL366947 | BRETAZENIL | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL49141 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL10483 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL301605 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3144617 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL267665 | RO-147437 | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL307202 | — | Ki | = | 2.08 | nM | 8.68 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL6597 | Ro-154513 | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL10534 | — | Ki | = | 2.79 | nM | 8.55 |
| CHEMBL173329 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3144795 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1518572 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL11709 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL10195 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL57655 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL17468 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL368768 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL133272 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL79945 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL6655 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL6659 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL173193 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL141039 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL336728 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL439945 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL341398 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL173339 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL454095 | ABECARNIL | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL307783 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL69719 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL415290 | Ro-151310 | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL177076 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL85861 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL12 | DIAZEPAM | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL415293 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL286594 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL6421 | — | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL59180 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL173938 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL299250 | — | Ki | = | 25.1 | nM | 7.60 |