Assay Detail
Binding
CHEMBL681405
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human gamma-amino butyric-acid A receptor alpha-2-beta-3-gamma-2, using a [3H]-Ro- 15-1788 radioligand
31
Total Activities
31
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.46 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17547 | — | — | 1 | 8.28 |
| CHEMBL69946 | — | — | 1 | 8.12 |
| CHEMBL275645 | — | — | 1 | 7.92 |
| CHEMBL17468 | — | — | 1 | 7.89 |
| CHEMBL17603 | — | — | 1 | 7.80 |
| CHEMBL274281 | — | — | 1 | 7.80 |
| CHEMBL308481 | — | — | 1 | 7.72 |
| CHEMBL17466 | — | — | 1 | 7.68 |
| CHEMBL17698 | — | — | 1 | 7.58 |
| CHEMBL308077 | — | — | 1 | 7.55 |
| CHEMBL17574 | — | — | 1 | 7.51 |
| CHEMBL73486 | — | — | 1 | 7.41 |
| CHEMBL276508 | — | — | 1 | 7.37 |
| CHEMBL277504 | — | — | 1 | 7.36 |
| CHEMBL312118 | — | — | 1 | 7.36 |
| CHEMBL302979 | — | — | 1 | 7.34 |
| CHEMBL420929 | — | — | 1 | 7.32 |
| CHEMBL432542 | — | — | 1 | 7.31 |
| CHEMBL17354 | — | — | 1 | 7.25 |
| CHEMBL72914 | — | — | 1 | 6.79 |
| CHEMBL73052 | — | — | 1 | 6.79 |
| CHEMBL70526 | — | — | 1 | 6.74 |
| CHEMBL70812 | — | — | 1 | 6.74 |
| CHEMBL304568 | — | — | 1 | - |
| CHEMBL72357 | — | — | 1 | - |
| CHEMBL69842 | — | — | 1 | - |
| CHEMBL70604 | — | — | 1 | - |
| CHEMBL307473 | — | — | 1 | - |
| CHEMBL69945 | — | — | 1 | - |
| CHEMBL71006 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17547 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL69946 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL275645 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL17468 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL17603 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL274281 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL308481 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL17466 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL17698 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL308077 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL17574 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL73486 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL276508 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL277504 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL312118 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL302979 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL420929 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL432542 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL17354 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL72914 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL73052 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL70526 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL70812 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL304568 | — | Ki | > | 300.0 | nM | - |
| CHEMBL72357 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69842 | — | Ki | > | 300.0 | nM | - |
| CHEMBL70604 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307473 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69945 | — | Ki | > | 300.0 | nM | - |
| CHEMBL71006 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307218 | — | Ki | > | 300.0 | nM | - |