Assay Detail
Binding
CHEMBL1058014
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Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABA receptor from rat cortical membrane by scintillation counting in absence of 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 | 4.55 | 5.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 5.21 |
| CHEMBL263127 | — | — | 1 | 4.81 |
| CHEMBL407094 | — | — | 1 | 4.68 |
| CHEMBL681 | ETOMIDATE | 4.0 | 1 | 4.42 |
| CHEMBL261379 | — | — | 1 | 4.10 |
| CHEMBL190279 | ALFAXALONE | 2.0 | 1 | 4.07 |
| CHEMBL406437 | — | — | 1 | - |
| CHEMBL261771 | — | — | 1 | - |
| CHEMBL405684 | — | — | 1 | - |
| CHEMBL260469 | — | — | 1 | - |
| CHEMBL260871 | — | — | 1 | - |
| CHEMBL406436 | — | — | 1 | - |
| CHEMBL406326 | — | — | 1 | - |
| CHEMBL261038 | — | — | 1 | - |
| CHEMBL259660 | — | — | 1 | - |
| CHEMBL406747 | — | — | 1 | - |
| CHEMBL261039 | — | — | 1 | - |
| CHEMBL260402 | IODOMETOMIDATE I-123, R- | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL263127 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL407094 | — | IC50 | = | 20700.0 | nM | 4.68 |
| CHEMBL681 | ETOMIDATE | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL261379 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL190279 | ALFAXALONE | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL406437 | — | IC50 | = | 163000.0 | nM | - |
| CHEMBL261771 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL405684 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL260469 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL260871 | — | IC50 | = | 111000.0 | nM | - |
| CHEMBL406436 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL406326 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL261038 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL259660 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL406747 | — | IC50 | = | 109000.0 | nM | - |
| CHEMBL261039 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL260402 | IODOMETOMIDATE I-123, R- | IC50 | > | 300000.0 | nM | - |