Assay Detail
Binding
CHEMBL2024697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]TBPS from GABAA receptor picrotoxin binding site in rat brain membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Neurosteroid analogues. 17. Inverted binding orientations of androsterone enantiomers at the steroid potentiation site on γ-aminobutyric acid type A receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.60 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2021957 | — | — | 1 | 7.82 |
| CHEMBL3138531 | — | — | 1 | 7.28 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.13 |
| CHEMBL429756 | — | — | 1 | 6.98 |
| CHEMBL3138532 | — | — | 1 | 6.78 |
| CHEMBL2021955 | — | — | 1 | 6.54 |
| CHEMBL3138446 | — | — | 1 | 6.51 |
| CHEMBL87285 | ANDROSTERONE | — | 1 | 6.39 |
| CHEMBL3138444 | — | — | 1 | 6.33 |
| CHEMBL3138534 | — | — | 1 | 5.69 |
| CHEMBL2021961 | — | — | 1 | 5.17 |
| CHEMBL3138533 | — | — | 1 | - |
| CHEMBL2021959 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2021957 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3138531 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL429756 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL3138532 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL2021955 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL3138446 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL87285 | ANDROSTERONE | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3138444 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL3138534 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL2021961 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL3138533 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2021959 | — | IC50 | > | 10000.0 | nM | - |