Assay Detail
Binding
CHEMBL682253
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-3-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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 7.40 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275645 | — | — | 1 | 8.15 |
| CHEMBL17468 | — | — | 1 | 8.12 |
| CHEMBL17547 | — | — | 1 | 8.00 |
| CHEMBL274281 | — | — | 1 | 7.80 |
| CHEMBL69946 | — | — | 1 | 7.75 |
| CHEMBL17603 | — | — | 1 | 7.70 |
| CHEMBL17354 | — | — | 1 | 7.68 |
| CHEMBL17466 | — | — | 1 | 7.62 |
| CHEMBL17698 | — | — | 1 | 7.60 |
| CHEMBL73486 | — | — | 1 | 7.55 |
| CHEMBL17574 | — | — | 1 | 7.48 |
| CHEMBL276508 | — | — | 1 | 7.46 |
| CHEMBL308077 | — | — | 1 | 7.39 |
| CHEMBL277504 | — | — | 1 | 7.33 |
| CHEMBL308481 | — | — | 1 | 7.32 |
| CHEMBL420929 | — | — | 1 | 7.32 |
| CHEMBL302979 | — | — | 1 | 7.30 |
| CHEMBL70526 | — | — | 1 | 7.16 |
| CHEMBL312118 | — | — | 1 | 7.06 |
| CHEMBL432542 | — | — | 1 | 6.99 |
| CHEMBL73052 | — | — | 1 | 6.80 |
| CHEMBL70812 | — | — | 1 | 6.74 |
| CHEMBL72357 | — | — | 1 | 6.73 |
| CHEMBL72914 | — | — | 1 | 6.62 |
| CHEMBL304568 | — | — | 1 | - |
| CHEMBL69842 | — | — | 1 | - |
| CHEMBL70604 | — | — | 1 | - |
| CHEMBL71006 | — | — | 1 | - |
| CHEMBL307473 | — | — | 1 | - |
| CHEMBL69945 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275645 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL17468 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL17547 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL274281 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL69946 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL17603 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL17354 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL17466 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL17698 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL73486 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL17574 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL276508 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL308077 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL277504 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL308481 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL420929 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL302979 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL70526 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL312118 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL432542 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL73052 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL70812 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL72357 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL72914 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL304568 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69842 | — | Ki | > | 300.0 | nM | - |
| CHEMBL70604 | — | Ki | > | 300.0 | nM | - |
| CHEMBL71006 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307473 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69945 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307218 | — | Ki | > | 300.0 | nM | - |