Assay Detail
Binding
CHEMBL681641
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Binding affinity to human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2, determined using [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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 7.41 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17547 | — | — | 1 | 8.44 |
| CHEMBL308481 | — | — | 1 | 8.37 |
| CHEMBL275645 | — | — | 1 | 8.30 |
| CHEMBL69946 | — | — | 1 | 8.00 |
| CHEMBL17468 | — | — | 1 | 8.00 |
| CHEMBL274281 | — | — | 1 | 7.92 |
| CHEMBL17603 | — | — | 1 | 7.70 |
| CHEMBL308077 | — | — | 1 | 7.66 |
| CHEMBL73486 | — | — | 1 | 7.62 |
| CHEMBL17466 | — | — | 1 | 7.51 |
| CHEMBL17698 | — | — | 1 | 7.35 |
| CHEMBL70812 | — | — | 1 | 7.24 |
| CHEMBL302979 | — | — | 1 | 7.22 |
| CHEMBL277504 | — | — | 1 | 7.21 |
| CHEMBL17354 | — | — | 1 | 7.18 |
| CHEMBL312118 | — | — | 1 | 7.14 |
| CHEMBL420929 | — | — | 1 | 7.10 |
| CHEMBL70526 | — | — | 1 | 6.92 |
| CHEMBL17574 | — | — | 1 | 6.78 |
| CHEMBL276508 | — | — | 1 | 6.76 |
| CHEMBL73052 | — | — | 1 | 6.76 |
| CHEMBL72914 | — | — | 1 | 6.68 |
| CHEMBL432542 | — | — | 1 | 6.57 |
| CHEMBL72357 | — | — | 1 | - |
| CHEMBL304568 | — | — | 1 | - |
| CHEMBL307473 | — | — | 1 | - |
| CHEMBL69842 | — | — | 1 | - |
| CHEMBL70604 | — | — | 1 | - |
| CHEMBL71006 | — | — | 1 | - |
| CHEMBL69945 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17547 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL308481 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL275645 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL69946 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL17468 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL274281 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL17603 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL308077 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL73486 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL17466 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL17698 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL70812 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL302979 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL277504 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL17354 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL312118 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL420929 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL70526 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL17574 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL276508 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL73052 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL72914 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL432542 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL72357 | — | Ki | > | 300.0 | nM | - |
| CHEMBL304568 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307473 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69842 | — | Ki | > | 300.0 | nM | - |
| CHEMBL70604 | — | Ki | > | 300.0 | nM | - |
| CHEMBL71006 | — | Ki | > | 300.0 | nM | - |
| CHEMBL69945 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307218 | — | Ki | > | 300.0 | nM | - |