Assay Detail
Binding
CHEMBL682709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells
36
Total Activities
36
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
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.49 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416659 | — | — | 1 | 9.00 |
| CHEMBL68490 | — | — | 1 | 8.80 |
| CHEMBL68684 | — | — | 1 | 8.57 |
| CHEMBL120838 | — | — | 1 | 8.54 |
| CHEMBL122154 | — | — | 1 | 8.46 |
| CHEMBL121277 | — | — | 1 | 8.24 |
| CHEMBL121275 | — | — | 1 | 8.07 |
| CHEMBL122619 | — | — | 1 | 8.01 |
| CHEMBL121370 | — | — | 1 | 7.81 |
| CHEMBL305068 | — | — | 1 | 7.78 |
| CHEMBL121088 | — | — | 1 | 7.78 |
| CHEMBL123406 | — | — | 1 | 7.71 |
| CHEMBL52030 | — | — | 1 | 7.65 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.58 |
| CHEMBL121603 | — | — | 1 | 7.55 |
| CHEMBL331569 | — | — | 1 | 7.54 |
| CHEMBL332893 | — | — | 1 | 7.47 |
| CHEMBL334246 | — | — | 1 | 7.45 |
| CHEMBL334138 | — | — | 1 | 7.42 |
| CHEMBL68712 | — | — | 1 | 7.35 |
| CHEMBL123530 | — | — | 1 | 7.24 |
| CHEMBL62630 | — | — | 1 | 7.20 |
| CHEMBL331907 | — | — | 1 | 7.18 |
| CHEMBL123882 | — | — | 1 | 7.17 |
| CHEMBL303718 | — | — | 1 | 7.07 |
| CHEMBL307230 | — | — | 1 | 6.96 |
| CHEMBL421257 | — | — | 1 | 6.78 |
| CHEMBL123471 | — | — | 1 | 6.69 |
| CHEMBL123072 | — | — | 1 | 6.68 |
| CHEMBL331657 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416659 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL68490 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL68684 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL120838 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL122154 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL121277 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL121275 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL122619 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL121370 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL121088 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL305068 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL123406 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL52030 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL12 | DIAZEPAM | Ki | = | 26.2 | nM | 7.58 |
| CHEMBL121603 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL331569 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL332893 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL334246 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL334138 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL68712 | — | Ki | = | 44.5 | nM | 7.35 |
| CHEMBL123530 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL62630 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL331907 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL123882 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL303718 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL307230 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL421257 | — | Ki | = | 166.3 | nM | 6.78 |
| CHEMBL123471 | — | Ki | = | 203.3 | nM | 6.69 |
| CHEMBL123072 | — | Ki | = | 208.8 | nM | 6.68 |
| CHEMBL331657 | — | Ki | = | 227.3 | nM | 6.64 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 255.1 | nM | 6.59 |
| CHEMBL421072 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL54859 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL331549 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL333659 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123078 | — | Ki | > | 1000.0 | nM | - |