Assay Detail
Binding
CHEMBL1058013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABAA receptor from rat cortical membrane by scintillation counting in presence of 1 uM GABA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.30 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 6.85 |
| CHEMBL190279 | ALFAXALONE | 2.0 | 1 | 6.05 |
| CHEMBL263127 | — | — | 1 | 5.89 |
| CHEMBL407094 | — | — | 1 | 5.83 |
| CHEMBL681 | ETOMIDATE | 4.0 | 1 | 5.69 |
| CHEMBL261379 | — | — | 1 | 5.32 |
| CHEMBL260871 | — | — | 1 | 5.15 |
| CHEMBL406747 | — | — | 1 | 5.12 |
| CHEMBL406437 | — | — | 1 | 5.05 |
| CHEMBL259660 | — | — | 1 | 4.81 |
| CHEMBL261039 | — | — | 1 | 4.48 |
| CHEMBL260402 | IODOMETOMIDATE I-123, R- | 1.0 | 1 | 4.43 |
| CHEMBL261771 | — | — | 1 | 4.28 |
| CHEMBL261038 | — | — | 1 | - |
| CHEMBL406326 | — | — | 1 | - |
| CHEMBL406436 | — | — | 1 | - |
| CHEMBL260469 | — | — | 1 | - |
| CHEMBL405684 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL190279 | ALFAXALONE | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL263127 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL407094 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL681 | ETOMIDATE | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL261379 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL260871 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL406747 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL406437 | — | IC50 | = | 8970.0 | nM | 5.05 |
| CHEMBL259660 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL261039 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL260402 | IODOMETOMIDATE I-123, R- | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL261771 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL261038 | — | IC50 | = | 169000.0 | nM | - |
| CHEMBL406326 | — | IC50 | = | 157000.0 | nM | - |
| CHEMBL406436 | — | IC50 | = | 202000.0 | nM | - |
| CHEMBL260469 | — | IC50 | = | 155000.0 | nM | - |
| CHEMBL405684 | — | IC50 | = | 122000.0 | nM | - |