Assay Detail
Binding
CHEMBL867915
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Displacement of [35S]TBPS from GABA-A receptor in rat brain membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.13 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42983 | — | — | 1 | 7.30 |
| CHEMBL210952 | ELTANOLONE | 2.0 | 1 | 7.15 |
| CHEMBL209370 | — | — | 1 | 7.14 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.13 |
| CHEMBL379611 | — | — | 1 | 6.89 |
| CHEMBL212635 | — | — | 1 | 6.89 |
| CHEMBL87285 | ANDROSTERONE | — | 1 | 6.39 |
| CHEMBL377911 | — | — | 1 | 6.28 |
| CHEMBL377913 | — | — | 1 | 6.24 |
| CHEMBL209801 | — | — | 1 | 5.93 |
| CHEMBL380223 | — | — | 1 | 5.91 |
| CHEMBL436930 | — | — | 1 | 5.72 |
| CHEMBL211784 | — | — | 1 | 5.70 |
| CHEMBL214112 | — | — | 1 | 5.69 |
| CHEMBL211747 | — | — | 1 | 5.46 |
| CHEMBL212101 | — | — | 1 | 5.41 |
| CHEMBL85799 | ETIOCHOLANOLONE | — | 1 | 5.38 |
| CHEMBL211898 | — | — | 1 | 5.38 |
| CHEMBL379925 | — | — | 1 | 5.30 |
| CHEMBL376997 | — | — | 1 | 5.27 |
| CHEMBL213677 | — | — | 1 | - |
| CHEMBL214113 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42983 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL210952 | ELTANOLONE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL209370 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL379611 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL212635 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL87285 | ANDROSTERONE | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL377911 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL377913 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL209801 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL380223 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL436930 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL211784 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL214112 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL211747 | — | IC50 | = | 3510.0 | nM | 5.46 |
| CHEMBL212101 | — | IC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL85799 | ETIOCHOLANOLONE | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL211898 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL379925 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL376997 | — | IC50 | = | 5420.0 | nM | 5.27 |
| CHEMBL213677 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL214113 | — | IC50 | > | 30000.0 | nM | - |