Assay Detail
Binding
CHEMBL680071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes.
35
Total Activities
35
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
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.83 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL444045 | — | — | 1 | 8.21 |
| CHEMBL3137994 | — | — | 1 | 7.57 |
| CHEMBL3137972 | — | — | 1 | 7.43 |
| CHEMBL3137986 | — | — | 1 | 7.41 |
| CHEMBL3137997 | — | — | 1 | 7.40 |
| CHEMBL3138276 | — | — | 1 | 7.37 |
| CHEMBL3137983 | — | — | 1 | 7.30 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.29 |
| CHEMBL3137987 | — | — | 1 | 7.19 |
| CHEMBL3138282 | — | — | 1 | 7.15 |
| CHEMBL3138277 | — | — | 1 | 7.12 |
| CHEMBL1568698 | GANAXOLONE | 4.0 | 1 | 7.10 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.04 |
| CHEMBL3138281 | — | — | 1 | 6.92 |
| CHEMBL3137976 | — | — | 1 | 6.87 |
| CHEMBL3137995 | — | — | 1 | 6.76 |
| CHEMBL3137977 | — | — | 1 | 6.67 |
| CHEMBL3138280 | — | — | 1 | 6.65 |
| CHEMBL3137982 | — | — | 1 | 6.64 |
| CHEMBL3138284 | — | — | 1 | 6.64 |
| CHEMBL3137992 | — | — | 1 | 6.64 |
| CHEMBL3137993 | — | — | 1 | 6.61 |
| CHEMBL3138285 | — | — | 1 | 6.59 |
| CHEMBL3137990 | — | — | 1 | 6.58 |
| CHEMBL3137991 | — | — | 1 | 6.49 |
| CHEMBL3137989 | — | — | 1 | 6.44 |
| CHEMBL3137979 | — | — | 1 | 6.42 |
| CHEMBL3138435 | — | — | 1 | 6.21 |
| CHEMBL3137973 | — | — | 1 | 6.18 |
| CHEMBL3138275 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL444045 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3137994 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3137972 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3137986 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3137997 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3138276 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3137983 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3137987 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3138282 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3138277 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1568698 | GANAXOLONE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3138281 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3137976 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3137995 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3137977 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3138280 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL3138284 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3137992 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL3137982 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL3137993 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL3138285 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3137990 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3137991 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL3137989 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3137979 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL3138435 | — | IC50 | = | 614.0 | nM | 6.21 |
| CHEMBL3137973 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL3138275 | — | IC50 | = | 702.0 | nM | 6.15 |
| CHEMBL448 | PENTOBARBITAL | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3137988 | — | IC50 | = | 2134.0 | nM | 5.67 |
| CHEMBL3137996 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3137984 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3137998 | — | IC50 | > | 10000.0 | nM | - |