Assay Detail
Binding
CHEMBL682716
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Inhibition of [35S]TBPS binding to GABA-A receptor in rat cerebral cortex.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.21 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190279 | ALFAXALONE | 2.0 | 1 | 6.52 |
| CHEMBL298951 | — | — | 1 | 6.07 |
| CHEMBL54497 | — | — | 1 | 5.97 |
| CHEMBL53267 | — | — | 1 | 5.92 |
| CHEMBL292402 | — | — | 1 | 5.84 |
| CHEMBL299111 | — | — | 1 | 5.71 |
| CHEMBL526 | PROPOFOL | 4.0 | 1 | 5.40 |
| CHEMBL55354 | — | — | 1 | 5.24 |
| CHEMBL55136 | — | — | 1 | 5.24 |
| CHEMBL55280 | — | — | 1 | 5.19 |
| CHEMBL56587 | — | — | 1 | 5.07 |
| CHEMBL52652 | — | — | 1 | 5.03 |
| CHEMBL52991 | — | — | 1 | 4.85 |
| CHEMBL55916 | — | — | 1 | 4.82 |
| CHEMBL52519 | — | — | 1 | 4.81 |
| CHEMBL52707 | — | — | 1 | 4.66 |
| CHEMBL57165 | — | — | 1 | 4.63 |
| CHEMBL434788 | — | — | 1 | 4.43 |
| CHEMBL430581 | — | — | 1 | 4.40 |
| CHEMBL448 | PENTOBARBITAL | 4.0 | 1 | 4.40 |
| CHEMBL300593 | — | — | 1 | - |
| CHEMBL55756 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190279 | ALFAXALONE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL298951 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL54497 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL53267 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL292402 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL299111 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL526 | PROPOFOL | IC50 | = | 3950.0 | nM | 5.40 |
| CHEMBL55354 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL55136 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL55280 | — | IC50 | = | 6520.0 | nM | 5.19 |
| CHEMBL56587 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL52652 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL52991 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL55916 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL52519 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL52707 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL57165 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL434788 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL430581 | — | IC50 | = | 39500.0 | nM | 4.40 |
| CHEMBL448 | PENTOBARBITAL | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL300593 | — | IC50 | = | 131000.0 | nM | - |
| CHEMBL55756 | — | IC50 | = | 739000.0 | nM | - |