Assay Detail
Binding
CHEMBL677034
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Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor 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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 7.20 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68490 | — | — | 1 | 9.06 |
| CHEMBL68684 | — | — | 1 | 8.85 |
| CHEMBL416659 | — | — | 1 | 8.72 |
| CHEMBL122154 | — | — | 1 | 8.38 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.84 |
| CHEMBL120838 | — | — | 1 | 7.76 |
| CHEMBL121277 | — | — | 1 | 7.57 |
| CHEMBL121275 | — | — | 1 | 7.55 |
| CHEMBL331569 | — | — | 1 | 7.37 |
| CHEMBL52030 | — | — | 1 | 7.31 |
| CHEMBL122619 | — | — | 1 | 7.31 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.28 |
| CHEMBL123406 | — | — | 1 | 7.24 |
| CHEMBL121088 | — | — | 1 | 7.23 |
| CHEMBL121370 | — | — | 1 | 7.13 |
| CHEMBL305068 | — | — | 1 | 7.12 |
| CHEMBL121603 | — | — | 1 | 7.08 |
| CHEMBL331907 | — | — | 1 | 6.94 |
| CHEMBL68712 | — | — | 1 | 6.91 |
| CHEMBL334138 | — | — | 1 | 6.83 |
| CHEMBL334246 | — | — | 1 | 6.80 |
| CHEMBL332893 | — | — | 1 | 6.77 |
| CHEMBL62630 | — | — | 1 | 6.60 |
| CHEMBL307230 | — | — | 1 | 6.57 |
| CHEMBL123530 | — | — | 1 | 6.55 |
| CHEMBL303718 | — | — | 1 | 6.55 |
| CHEMBL331657 | — | — | 1 | 6.29 |
| CHEMBL421072 | — | — | 1 | 6.00 |
| CHEMBL54859 | — | — | 1 | 5.19 |
| CHEMBL333659 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68490 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL68684 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL416659 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL122154 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL12 | DIAZEPAM | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL120838 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL121277 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL121275 | — | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL331569 | — | Ki | = | 42.9 | nM | 7.37 |
| CHEMBL122619 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL52030 | — | Ki | = | 48.5 | nM | 7.31 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 52.1 | nM | 7.28 |
| CHEMBL123406 | — | Ki | = | 57.7 | nM | 7.24 |
| CHEMBL121088 | — | Ki | = | 58.5 | nM | 7.23 |
| CHEMBL121370 | — | Ki | = | 74.3 | nM | 7.13 |
| CHEMBL305068 | — | Ki | = | 75.7 | nM | 7.12 |
| CHEMBL121603 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL331907 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL68712 | — | Ki | = | 122.2 | nM | 6.91 |
| CHEMBL334138 | — | Ki | = | 147.3 | nM | 6.83 |
| CHEMBL334246 | — | Ki | = | 158.6 | nM | 6.80 |
| CHEMBL332893 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL62630 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL307230 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL123530 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL303718 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL331657 | — | Ki | = | 518.0 | nM | 6.29 |
| CHEMBL421072 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL54859 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL333659 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123072 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL331549 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL421257 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123078 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123882 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL123471 | — | Ki | > | 1000.0 | nM | - |