Assay Detail
Binding
CHEMBL992851
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from human recombinant GABAA alpha-1-beta-2-gamma-2S receptor expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABA(A) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 9.14 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487686 | — | — | 1 | 9.92 |
| CHEMBL488283 | — | — | 1 | 9.92 |
| CHEMBL469477 | — | — | 1 | 9.92 |
| CHEMBL487687 | — | — | 1 | 9.85 |
| CHEMBL381059 | — | — | 1 | 9.57 |
| CHEMBL471551 | — | — | 1 | 9.42 |
| CHEMBL487685 | — | — | 1 | 9.41 |
| CHEMBL520411 | — | — | 1 | 9.29 |
| CHEMBL488284 | — | — | 1 | 9.28 |
| CHEMBL487688 | — | — | 1 | 9.06 |
| CHEMBL470283 | — | — | 1 | 9.01 |
| CHEMBL488286 | — | — | 1 | 8.57 |
| CHEMBL488285 | — | — | 1 | 8.49 |
| CHEMBL506314 | — | — | 1 | 8.29 |
| CHEMBL206540 | — | — | 1 | 8.23 |
| CHEMBL487867 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487686 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL488283 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL469477 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL487687 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL381059 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL471551 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL487685 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL520411 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL488284 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL487688 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL470283 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL488286 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL488285 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL506314 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL206540 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL487867 | — | Ki | = | 11.0 | nM | 7.96 |