Assay Detail
Binding
CHEMBL681273
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of tert-butyl bicyclophosphorothionate ([35 S]TBPS) at Gamma-aminobutyric acid A receptor from rat whole brain membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Conformationally constrained anesthetic steroids that modulate GABA(A) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.34 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429756 | — | — | 1 | 7.26 |
| CHEMBL210952 | ELTANOLONE | 2.0 | 1 | 6.84 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 6.81 |
| CHEMBL133736 | — | — | 1 | 6.80 |
| CHEMBL1256760 | — | — | 1 | 6.72 |
| CHEMBL422984 | — | — | 1 | 6.68 |
| CHEMBL510813 | — | — | 1 | 6.66 |
| CHEMBL130165 | — | — | 1 | 6.63 |
| CHEMBL337881 | — | — | 1 | 6.59 |
| CHEMBL190279 | ALFAXALONE | 2.0 | 1 | 6.37 |
| CHEMBL341185 | — | — | 1 | 5.91 |
| CHEMBL87285 | ANDROSTERONE | — | 1 | 5.86 |
| CHEMBL422795 | — | — | 1 | 5.75 |
| CHEMBL335062 | ANDROSTANDIOL | — | 1 | 5.73 |
| CHEMBL334621 | — | — | 1 | 5.60 |
| CHEMBL336207 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429756 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL210952 | ELTANOLONE | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL133736 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL1256760 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL422984 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL510813 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL130165 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL337881 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL190279 | ALFAXALONE | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL341185 | — | IC50 | = | 1236.0 | nM | 5.91 |
| CHEMBL87285 | ANDROSTERONE | IC50 | = | 1367.0 | nM | 5.86 |
| CHEMBL422795 | — | IC50 | = | 1767.0 | nM | 5.75 |
| CHEMBL335062 | ANDROSTANDIOL | IC50 | = | 1867.0 | nM | 5.73 |
| CHEMBL334621 | — | IC50 | = | 2533.0 | nM | 5.60 |
| CHEMBL336207 | — | IC50 | = | 5350.0 | nM | 5.27 |