Assay Detail
Binding
CHEMBL680669
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Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells
35
Total Activities
35
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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 35 | 8.34 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122619 | — | — | 1 | 9.41 |
| CHEMBL120838 | — | — | 1 | 9.36 |
| CHEMBL52030 | — | — | 1 | 9.35 |
| CHEMBL121275 | — | — | 1 | 9.11 |
| CHEMBL68490 | — | — | 1 | 9.10 |
| CHEMBL68684 | — | — | 1 | 9.10 |
| CHEMBL331569 | — | — | 1 | 9.04 |
| CHEMBL121277 | — | — | 1 | 9.03 |
| CHEMBL121088 | — | — | 1 | 9.00 |
| CHEMBL416659 | — | — | 1 | 8.89 |
| CHEMBL305068 | — | — | 1 | 8.85 |
| CHEMBL121603 | — | — | 1 | 8.74 |
| CHEMBL123072 | — | — | 1 | 8.68 |
| CHEMBL68712 | — | — | 1 | 8.52 |
| CHEMBL62630 | — | — | 1 | 8.51 |
| CHEMBL421257 | — | — | 1 | 8.48 |
| CHEMBL332893 | — | — | 1 | 8.46 |
| CHEMBL307230 | — | — | 1 | 8.43 |
| CHEMBL334246 | — | — | 1 | 8.42 |
| CHEMBL121370 | — | — | 1 | 8.41 |
| CHEMBL331907 | — | — | 1 | 8.40 |
| CHEMBL303718 | — | — | 1 | 8.34 |
| CHEMBL123406 | — | — | 1 | 8.26 |
| CHEMBL123882 | — | — | 1 | 8.19 |
| CHEMBL123530 | — | — | 1 | 8.17 |
| CHEMBL334138 | — | — | 1 | 8.05 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.95 |
| CHEMBL421072 | — | — | 1 | 7.89 |
| CHEMBL331657 | — | — | 1 | 7.82 |
| CHEMBL123471 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122619 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL120838 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL52030 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL121275 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL68490 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL68684 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL331569 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL121277 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL121088 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL416659 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL305068 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL121603 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL123072 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL68712 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL62630 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL421257 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL332893 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL307230 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL334246 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL121370 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL331907 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL303718 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL123406 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL123882 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL123530 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL334138 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL12 | DIAZEPAM | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL421072 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL331657 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL123471 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL331549 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL123078 | — | Ki | = | 213.7 | nM | 6.67 |
| CHEMBL333659 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL54859 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL911 | ZOLPIDEM | Ki | > | 10000.0 | nM | - |