Assay Detail
Binding
CHEMBL3058331
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Ro 15-1788 from Homo sapiens (human) recombinant GABAA alpha2beta3gamma2 receptor expressed in Ltk- cells after 1 hr by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ltk- |
| 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
Development of Selective Ligands for Benzodiazepine Receptor Subtypes by Manipulating the Substituents at Positions 3- and 7- of Optically Active BzR Ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.24 | 7.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2261918 | — | — | 1 | 7.79 |
| CHEMBL52030 | — | — | 1 | 7.56 |
| CHEMBL336377 | — | — | 1 | 7.54 |
| CHEMBL2261632 | — | — | 1 | 7.47 |
| CHEMBL2261919 | — | — | 1 | 7.46 |
| CHEMBL339163 | — | — | 1 | 7.36 |
| CHEMBL2261631 | — | — | 1 | 7.26 |
| CHEMBL2261633 | — | — | 1 | 7.26 |
| CHEMBL2261917 | — | — | 1 | 6.92 |
| CHEMBL129855 | — | — | 1 | 6.91 |
| CHEMBL2261922 | — | — | 1 | 6.91 |
| CHEMBL2261916 | — | — | 1 | 6.89 |
| CHEMBL2261634 | — | — | 1 | 6.76 |
| CHEMBL2261915 | — | — | 1 | - |
| CHEMBL2261920 | — | — | 1 | - |
| CHEMBL2261921 | — | — | 1 | - |
| CHEMBL2261923 | — | — | 1 | - |
| CHEMBL2261630 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2261918 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL52030 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL336377 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2261632 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2261919 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL339163 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2261631 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2261633 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2261917 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL129855 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL2261922 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL2261916 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL2261634 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL2261915 | — | Ki | > | 333.0 | nM | - |
| CHEMBL2261920 | — | Ki | > | 333.0 | nM | - |
| CHEMBL2261921 | — | Ki | > | 333.0 | nM | - |
| CHEMBL2261923 | — | Ki | > | 333.0 | nM | - |
| CHEMBL2261630 | — | Ki | > | 333.0 | nM | - |