Assay Detail
Binding
CHEMBL676826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 62 | 7.32 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299210 | — | — | 1 | 9.29 |
| CHEMBL300615 | — | — | 1 | 9.09 |
| CHEMBL300951 | — | — | 1 | 8.92 |
| CHEMBL300862 | — | — | 1 | 8.70 |
| CHEMBL296607 | — | — | 1 | 8.66 |
| CHEMBL292380 | — | — | 1 | 8.64 |
| CHEMBL298386 | — | — | 1 | 8.62 |
| CHEMBL299611 | — | — | 1 | 8.57 |
| CHEMBL292462 | — | — | 1 | 8.41 |
| CHEMBL53238 | — | — | 1 | 8.37 |
| CHEMBL300497 | — | — | 1 | 8.32 |
| CHEMBL416659 | — | — | 1 | 8.08 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.85 |
| CHEMBL301063 | — | — | 1 | 7.80 |
| CHEMBL50402 | — | — | 1 | 7.75 |
| CHEMBL441612 | — | — | 1 | 7.75 |
| CHEMBL50320 | — | — | 1 | 7.75 |
| CHEMBL299437 | — | — | 1 | 7.72 |
| CHEMBL52672 | — | — | 1 | 7.62 |
| CHEMBL52310 | — | — | 1 | 7.58 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.57 |
| CHEMBL296383 | — | — | 1 | 7.50 |
| CHEMBL55450 | — | — | 1 | 7.50 |
| CHEMBL273456 | — | — | 1 | 7.42 |
| CHEMBL301181 | — | — | 1 | 7.39 |
| CHEMBL52030 | — | — | 1 | 7.36 |
| CHEMBL299802 | — | — | 1 | 7.31 |
| CHEMBL299642 | — | — | 1 | 7.25 |
| CHEMBL298760 | — | — | 1 | 7.25 |
| CHEMBL13662 | CI-218872 | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299210 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL300615 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL300951 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL300862 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL296607 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL292380 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL298386 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL299611 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL292462 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL53238 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL300497 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL416659 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL12 | DIAZEPAM | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL301063 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL50320 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL441612 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL50402 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL299437 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL52672 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL52310 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL296383 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL55450 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL273456 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL301181 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL52030 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL299802 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL299642 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL298760 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL13662 | CI-218872 | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL53587 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL300018 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL51911 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL441978 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL53529 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL300867 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL445358 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL299736 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL298501 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL301336 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL50581 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL297481 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL54211 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL52696 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL297958 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL300690 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL53642 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL52640 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL53729 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL52818 | — | Ki | = | 960.0 | nM | 6.02 |