Assay Detail
Binding
CHEMBL888744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]TBPS from GABAA receptor in Sprague-Dawley rat cortex membrane
44
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Enaminone amides as novel orally active GABAA receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.85 | 8.15 |
| Imax | 22 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426916 | — | — | 2 | 8.15 |
| CHEMBL387622 | — | — | 2 | 8.10 |
| CHEMBL390326 | — | — | 2 | 7.70 |
| CHEMBL387958 | — | — | 2 | 7.52 |
| CHEMBL229535 | — | — | 2 | 7.52 |
| CHEMBL229534 | — | — | 2 | 7.40 |
| CHEMBL556727 | — | — | 2 | 7.35 |
| CHEMBL229374 | — | — | 2 | 7.30 |
| CHEMBL229201 | — | — | 2 | 7.10 |
| CHEMBL226962 | — | — | 2 | 7.05 |
| CHEMBL226908 | — | — | 2 | 6.89 |
| CHEMBL227018 | — | — | 2 | 6.80 |
| CHEMBL226909 | — | — | 2 | 6.52 |
| CHEMBL226965 | — | — | 2 | 6.44 |
| CHEMBL388639 | — | — | 2 | 6.40 |
| CHEMBL226964 | — | — | 2 | 6.35 |
| CHEMBL226910 | — | — | 2 | 6.31 |
| CHEMBL226963 | — | — | 2 | 6.22 |
| CHEMBL387621 | — | — | 2 | 6.16 |
| CHEMBL375684 | — | — | 2 | 6.05 |
| CHEMBL227017 | — | — | 2 | 5.77 |
| CHEMBL388638 | — | — | 2 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426916 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL387622 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL390326 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL387958 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL229535 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL229534 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL556727 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL229374 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL229201 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL226962 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL226908 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL227018 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL226909 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL226965 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL388639 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL226964 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL226910 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL226963 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL387621 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL375684 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL227017 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL388638 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL226908 | — | Imax | = | 87.0 | % | - |
| CHEMBL388639 | — | Imax | = | 94.0 | % | - |
| CHEMBL388638 | — | Imax | = | 100.0 | % | - |
| CHEMBL229201 | — | Imax | = | 86.0 | % | - |
| CHEMBL387958 | — | Imax | = | 88.0 | % | - |
| CHEMBL426916 | — | Imax | = | 88.0 | % | - |
| CHEMBL229535 | — | Imax | = | 92.0 | % | - |
| CHEMBL390326 | — | Imax | = | 86.0 | % | - |
| CHEMBL229534 | — | Imax | = | 80.0 | % | - |
| CHEMBL556727 | — | Imax | = | 90.0 | % | - |
| CHEMBL227018 | — | Imax | = | 74.0 | % | - |
| CHEMBL227017 | — | Imax | = | 40.0 | % | - |
| CHEMBL387622 | — | Imax | = | 100.0 | % | - |
| CHEMBL226965 | — | Imax | = | 94.0 | % | - |
| CHEMBL226964 | — | Imax | = | 93.0 | % | - |
| CHEMBL375684 | — | Imax | = | 90.0 | % | - |
| CHEMBL226963 | — | Imax | = | 100.0 | % | - |
| CHEMBL229374 | — | Imax | = | 82.0 | % | - |
| CHEMBL387621 | — | Imax | = | 100.0 | % | - |
| CHEMBL226910 | — | Imax | = | 100.0 | % | - |
| CHEMBL226962 | — | Imax | = | 95.0 | % | - |
| CHEMBL226909 | — | Imax | = | 93.0 | % | - |