Assay Detail
Binding
CHEMBL679569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [3H]-Ro- 15-1788 binding to Gamma-aminobutyric acid A receptor alpha in vitro in rat cortical membranes
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 6.59 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335086 | — | — | 1 | 9.05 |
| CHEMBL134408 | — | — | 1 | 8.21 |
| CHEMBL131798 | — | — | 1 | 8.11 |
| CHEMBL135896 | — | — | 1 | 8.01 |
| CHEMBL334427 | — | — | 1 | 7.92 |
| CHEMBL131632 | — | — | 1 | 7.00 |
| CHEMBL337443 | — | — | 1 | 6.89 |
| CHEMBL134732 | — | — | 1 | 6.75 |
| CHEMBL134840 | — | — | 1 | 6.75 |
| CHEMBL134291 | 6-METHYLFLAVONE | — | 1 | 6.75 |
| CHEMBL134627 | — | — | 1 | 6.66 |
| CHEMBL336559 | — | — | 1 | 6.41 |
| CHEMBL134539 | — | — | 1 | 6.32 |
| CHEMBL135066 | — | — | 1 | 6.21 |
| CHEMBL132035 | — | — | 1 | 6.16 |
| CHEMBL131928 | — | — | 1 | 6.15 |
| CHEMBL133949 | — | — | 1 | 6.14 |
| CHEMBL334355 | — | — | 1 | 6.09 |
| CHEMBL423166 | — | — | 1 | 6.00 |
| CHEMBL132423 | — | — | 1 | 5.92 |
| CHEMBL132422 | — | — | 1 | 5.58 |
| CHEMBL334769 | — | — | 1 | 5.52 |
| CHEMBL336568 | — | — | 1 | 5.44 |
| CHEMBL275638 | FLAVONE | 2.0 | 1 | 5.38 |
| CHEMBL133226 | — | — | 1 | 5.36 |
| CHEMBL134315 | — | — | 1 | - |
| CHEMBL132837 | — | — | 1 | - |
| CHEMBL132011 | — | — | 1 | - |
| CHEMBL134517 | — | — | 1 | - |
| CHEMBL131620 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335086 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL134408 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL131798 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL135896 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL334427 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL131632 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL337443 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL134732 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL134840 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL134291 | 6-METHYLFLAVONE | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL134627 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL336559 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL134539 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL135066 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL132035 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL131928 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL133949 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL334355 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL423166 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL132423 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL132422 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL334769 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL336568 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL275638 | FLAVONE | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL133226 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL135798 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL133402 | — | Ki | > | 1700.0 | nM | - |
| CHEMBL134381 | — | Ki | > | 1900.0 | nM | - |
| CHEMBL135171 | — | Ki | > | 1500.0 | nM | - |
| CHEMBL134430 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL134626 | — | Ki | > | 1700.0 | nM | - |
| CHEMBL134429 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL135634 | — | Ki | > | 1500.0 | nM | - |
| CHEMBL134119 | — | Ki | > | 1500.0 | nM | - |
| CHEMBL337069 | — | Ki | > | 1500.0 | nM | - |
| CHEMBL337912 | — | Ki | > | 2100.0 | nM | - |
| CHEMBL133668 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL131620 | — | Ki | > | 1700.0 | nM | - |
| CHEMBL134517 | — | Ki | > | 1700.0 | nM | - |
| CHEMBL132011 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL132837 | — | Ki | > | 1600.0 | nM | - |
| CHEMBL134315 | — | Ki | > | 1500.0 | nM | - |