Assay Detail
Binding
CHEMBL5609171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of extrasynaptic alpha4beta3delta GABA-A receptor (unknown origin) transfected in CHO cells assessed as potentiation of GABA-induced peak current amplitude at -80 mV holding potential preincubated for 30 secs followed by GABA stimulation for 2 secs by manual patch assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta (CHEMBL3430899) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC<sub>50</sub> and E<sub>max</sub> as PAM on GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.99 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5612649 | — | — | 1 | 8.00 |
| CHEMBL5613388 | — | — | 1 | 7.68 |
| CHEMBL5612974 | — | — | 1 | 7.64 |
| CHEMBL5612194 | — | — | 1 | 7.54 |
| CHEMBL5613759 | — | — | 1 | 7.46 |
| CHEMBL5613513 | — | — | 1 | 7.39 |
| CHEMBL5613307 | — | — | 1 | 7.38 |
| CHEMBL5612003 | — | — | 1 | 7.30 |
| CHEMBL5612080 | — | — | 1 | 7.25 |
| CHEMBL5614180 | — | — | 1 | 7.17 |
| CHEMBL5614206 | — | — | 1 | 7.12 |
| CHEMBL5612455 | — | — | 1 | 7.10 |
| CHEMBL5612679 | — | — | 1 | 7.05 |
| CHEMBL5612666 | — | — | 1 | 6.97 |
| CHEMBL5614143 | — | — | 1 | 6.95 |
| CHEMBL5612996 | — | — | 1 | 6.91 |
| CHEMBL5613589 | — | — | 1 | 6.90 |
| CHEMBL4105630 | ZURANOLONE | 4.0 | 1 | 6.87 |
| CHEMBL5612574 | — | — | 1 | 6.86 |
| CHEMBL5612909 | — | — | 1 | 6.82 |
| CHEMBL5614044 | — | — | 1 | 6.77 |
| CHEMBL5612380 | — | — | 1 | 6.69 |
| CHEMBL5612876 | — | — | 1 | 6.67 |
| CHEMBL5613795 | — | — | 1 | 6.62 |
| CHEMBL5612737 | — | — | 1 | 6.58 |
| CHEMBL5613780 | — | — | 1 | 6.57 |
| CHEMBL5612427 | — | — | 1 | 6.57 |
| CHEMBL5613435 | — | — | 1 | 6.52 |
| CHEMBL5613603 | — | — | 1 | 6.44 |
| CHEMBL5613854 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5612649 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5613388 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5612974 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5612194 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5613759 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5613513 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5613307 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5612003 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5612080 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5614180 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5614206 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5612455 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5612679 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5612666 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5614143 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5612996 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5613589 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4105630 | ZURANOLONE | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5612574 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL5612909 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5614044 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5612380 | — | EC50 | = | 203.0 | nM | 6.69 |
| CHEMBL5612876 | — | EC50 | = | 213.0 | nM | 6.67 |
| CHEMBL5613795 | — | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL5612737 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL5613780 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5612427 | — | EC50 | = | 268.0 | nM | 6.57 |
| CHEMBL5613435 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL5613603 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5613854 | — | EC50 | = | 1238.0 | nM | 5.91 |