Assay Detail
Binding
CHEMBL685339
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Binding affinity to human GABA A alpha-5-beta-3-gamma-2 receptor, 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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 8.14 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17547 | — | — | 1 | 9.30 |
| CHEMBL308481 | — | — | 1 | 8.85 |
| CHEMBL73486 | — | — | 1 | 8.85 |
| CHEMBL274281 | — | — | 1 | 8.80 |
| CHEMBL17603 | — | — | 1 | 8.80 |
| CHEMBL17698 | — | — | 1 | 8.77 |
| CHEMBL275645 | — | — | 1 | 8.70 |
| CHEMBL277504 | — | — | 1 | 8.66 |
| CHEMBL17468 | — | — | 1 | 8.66 |
| CHEMBL69946 | — | — | 1 | 8.62 |
| CHEMBL17466 | — | — | 1 | 8.54 |
| CHEMBL312118 | — | — | 1 | 8.41 |
| CHEMBL308077 | — | — | 1 | 8.34 |
| CHEMBL302979 | — | — | 1 | 8.33 |
| CHEMBL420929 | — | — | 1 | 8.33 |
| CHEMBL17354 | — | — | 1 | 8.28 |
| CHEMBL17574 | — | — | 1 | 8.24 |
| CHEMBL276508 | — | — | 1 | 8.04 |
| CHEMBL72914 | — | — | 1 | 7.96 |
| CHEMBL70526 | — | — | 1 | 7.82 |
| CHEMBL73052 | — | — | 1 | 7.82 |
| CHEMBL70812 | — | — | 1 | 7.75 |
| CHEMBL432542 | — | — | 1 | 7.72 |
| CHEMBL72357 | — | — | 1 | 7.43 |
| CHEMBL69945 | — | — | 1 | 7.17 |
| CHEMBL70604 | — | — | 1 | 7.11 |
| CHEMBL71006 | — | — | 1 | 7.07 |
| CHEMBL69842 | — | — | 1 | 6.88 |
| CHEMBL304568 | — | — | 1 | 6.77 |
| CHEMBL307473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17547 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL308481 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL73486 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL274281 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL17603 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL17698 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL275645 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL277504 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL17468 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL69946 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL17466 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL312118 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL308077 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL302979 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL420929 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL17354 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL17574 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL276508 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL72914 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL70526 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL73052 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL70812 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL432542 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL72357 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL69945 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL70604 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL71006 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL69842 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL304568 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL307473 | — | Ki | > | 300.0 | nM | - |
| CHEMBL307218 | — | Ki | > | 300.0 | nM | - |