Assay Detail
Binding
CHEMBL681841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells
61
Total Activities
61
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| 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 | 61 | 7.42 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299210 | — | — | 1 | 9.15 |
| CHEMBL300862 | — | — | 1 | 8.80 |
| CHEMBL52672 | — | — | 1 | 8.77 |
| CHEMBL299611 | — | — | 1 | 8.77 |
| CHEMBL300951 | — | — | 1 | 8.74 |
| CHEMBL53238 | — | — | 1 | 8.72 |
| CHEMBL296607 | — | — | 1 | 8.66 |
| CHEMBL298386 | — | — | 1 | 8.64 |
| CHEMBL292380 | — | — | 1 | 8.54 |
| CHEMBL300497 | — | — | 1 | 8.44 |
| CHEMBL292462 | — | — | 1 | 8.43 |
| CHEMBL301063 | — | — | 1 | 8.24 |
| CHEMBL416659 | — | — | 1 | 8.10 |
| CHEMBL296383 | — | — | 1 | 8.01 |
| CHEMBL50402 | — | — | 1 | 7.96 |
| CHEMBL441612 | — | — | 1 | 7.80 |
| CHEMBL50581 | — | — | 1 | 7.80 |
| CHEMBL299437 | — | — | 1 | 7.80 |
| CHEMBL301181 | — | — | 1 | 7.77 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.70 |
| CHEMBL52030 | — | — | 1 | 7.66 |
| CHEMBL298760 | — | — | 1 | 7.62 |
| CHEMBL50320 | — | — | 1 | 7.60 |
| CHEMBL53587 | — | — | 1 | 7.58 |
| CHEMBL299802 | — | — | 1 | 7.55 |
| CHEMBL52310 | — | — | 1 | 7.42 |
| CHEMBL55450 | — | — | 1 | 7.40 |
| CHEMBL273456 | — | — | 1 | 7.39 |
| CHEMBL299642 | — | — | 1 | 7.36 |
| CHEMBL53529 | — | — | 1 | 7.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299210 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL300862 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL299611 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL52672 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL300951 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL53238 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL296607 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL298386 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL292380 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL300497 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL292462 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL301063 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL416659 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL296383 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL50402 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL441612 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL299437 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL50581 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL301181 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL12 | DIAZEPAM | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL52030 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL298760 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL50320 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL53587 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL299802 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL52310 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL55450 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL273456 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL299642 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL53529 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL441978 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL299736 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL300018 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL52640 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL300867 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL298501 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL301336 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL52696 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL53642 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL53729 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL300690 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL52818 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL445358 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL55081 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL51911 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL297717 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL54859 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL13662 | CI-218872 | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL273680 | — | Ki | > | 1000.0 | nM | - |