Assay Detail
Binding
CHEMBL829005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells
101
Total Activities
100
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
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 101 | 7.39 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361114 | — | — | 1 | 8.77 |
| CHEMBL179474 | — | — | 1 | 8.70 |
| CHEMBL360122 | — | — | 1 | 8.64 |
| CHEMBL361129 | — | — | 1 | 8.60 |
| CHEMBL179414 | — | — | 1 | 8.55 |
| CHEMBL178677 | — | — | 1 | 8.47 |
| CHEMBL361786 | — | — | 1 | 8.40 |
| CHEMBL179712 | — | — | 1 | 8.28 |
| CHEMBL179558 | — | — | 1 | 8.25 |
| CHEMBL179475 | — | — | 1 | 8.23 |
| CHEMBL178956 | — | — | 1 | 8.19 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.18 |
| CHEMBL366537 | — | — | 1 | 8.15 |
| CHEMBL362282 | — | — | 1 | 8.12 |
| CHEMBL178783 | — | — | 1 | 8.12 |
| CHEMBL179777 | — | — | 1 | 8.09 |
| CHEMBL369035 | — | — | 1 | 8.06 |
| CHEMBL180416 | — | — | 1 | 8.04 |
| CHEMBL175475 | — | — | 1 | 8.01 |
| CHEMBL362485 | — | — | 1 | 8.00 |
| CHEMBL180174 | — | — | 1 | 7.85 |
| CHEMBL361015 | — | — | 1 | 7.82 |
| CHEMBL366468 | — | — | 1 | 7.80 |
| CHEMBL178831 | — | — | 1 | 7.80 |
| CHEMBL178710 | — | — | 1 | 7.77 |
| CHEMBL361340 | — | — | 1 | 7.75 |
| CHEMBL360733 | — | — | 1 | 7.72 |
| CHEMBL359545 | — | — | 1 | 7.68 |
| CHEMBL360912 | — | — | 1 | 7.68 |
| CHEMBL175886 | — | — | 1 | 7.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361114 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL179474 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL360122 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL361129 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL179414 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL178677 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL361786 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL179712 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL179558 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL179475 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL178956 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL12 | DIAZEPAM | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL366537 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL178783 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL362282 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL179777 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL369035 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL180416 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL175475 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL362485 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL180174 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL361015 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL178831 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL366468 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL178710 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL361340 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL360733 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL360912 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL359545 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL175886 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL178738 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL359650 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL178942 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL362620 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL359906 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL178992 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL361200 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL179699 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL366471 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL68712 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL178242 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL178840 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL362409 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL178856 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL180464 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL179924 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL360966 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL361105 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL175929 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL440558 | — | Ki | = | 59.0 | nM | 7.23 |