Assay Detail
Binding
CHEMBL680432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 7.73 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416659 | — | — | 1 | 9.48 |
| CHEMBL68490 | — | — | 1 | 8.89 |
| CHEMBL68684 | — | — | 1 | 8.85 |
| CHEMBL122154 | — | — | 1 | 8.80 |
| CHEMBL120838 | — | — | 1 | 8.77 |
| CHEMBL121275 | — | — | 1 | 8.41 |
| CHEMBL331569 | — | — | 1 | 8.39 |
| CHEMBL121277 | — | — | 1 | 8.38 |
| CHEMBL121088 | — | — | 1 | 8.21 |
| CHEMBL122619 | — | — | 1 | 8.07 |
| CHEMBL121603 | — | — | 1 | 7.97 |
| CHEMBL305068 | — | — | 1 | 7.96 |
| CHEMBL121370 | — | — | 1 | 7.83 |
| CHEMBL123406 | — | — | 1 | 7.75 |
| CHEMBL334246 | — | — | 1 | 7.71 |
| CHEMBL332893 | — | — | 1 | 7.68 |
| CHEMBL331907 | — | — | 1 | 7.66 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.62 |
| CHEMBL68712 | — | — | 1 | 7.62 |
| CHEMBL52030 | — | — | 1 | 7.61 |
| CHEMBL123072 | — | — | 1 | 7.58 |
| CHEMBL334138 | — | — | 1 | 7.47 |
| CHEMBL62630 | — | — | 1 | 7.40 |
| CHEMBL303718 | — | — | 1 | 7.39 |
| CHEMBL123530 | — | — | 1 | 7.34 |
| CHEMBL307230 | — | — | 1 | 7.32 |
| CHEMBL421257 | — | — | 1 | 7.16 |
| CHEMBL123882 | — | — | 1 | 7.08 |
| CHEMBL331657 | — | — | 1 | 6.98 |
| CHEMBL421072 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416659 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL68490 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL68684 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL122154 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL120838 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL121275 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL331569 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL121277 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL121088 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL122619 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL121603 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL305068 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL121370 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL123406 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL334246 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL332893 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL331907 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL68712 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL12 | DIAZEPAM | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL52030 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL123072 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL334138 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL62630 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL303718 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL123530 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL307230 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL421257 | — | Ki | = | 69.6 | nM | 7.16 |
| CHEMBL123882 | — | Ki | = | 83.9 | nM | 7.08 |
| CHEMBL331657 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL421072 | — | Ki | = | 115.7 | nM | 6.94 |
| CHEMBL123471 | — | Ki | = | 226.9 | nM | 6.64 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 608.5 | nM | 6.22 |
| CHEMBL54859 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL331549 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL333659 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123078 | — | Ki | > | 1000.0 | nM | - |