Assay Detail
Binding
CHEMBL5609126
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of synaptic alpha1beta2gamma2 GABA-A receptor (unknown origin) transfected in LTK 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 Q-patch assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LTK |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| 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 | 6.72 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613388 | — | — | 1 | 7.58 |
| CHEMBL5612974 | — | — | 1 | 7.43 |
| CHEMBL5612649 | — | — | 1 | 7.25 |
| CHEMBL5612194 | — | — | 1 | 7.05 |
| CHEMBL5612080 | — | — | 1 | 6.96 |
| CHEMBL5612003 | — | — | 1 | 6.95 |
| CHEMBL5613307 | — | — | 1 | 6.90 |
| CHEMBL5612737 | — | — | 1 | 6.86 |
| CHEMBL5614206 | — | — | 1 | 6.85 |
| CHEMBL5612909 | — | — | 1 | 6.84 |
| CHEMBL4105630 | ZURANOLONE | 4.0 | 1 | 6.82 |
| CHEMBL5613759 | — | — | 1 | 6.81 |
| CHEMBL5612996 | — | — | 1 | 6.79 |
| CHEMBL5612666 | — | — | 1 | 6.77 |
| CHEMBL5613513 | — | — | 1 | 6.74 |
| CHEMBL5612380 | — | — | 1 | 6.72 |
| CHEMBL5613780 | — | — | 1 | 6.72 |
| CHEMBL5614044 | — | — | 1 | 6.66 |
| CHEMBL5612574 | — | — | 1 | 6.62 |
| CHEMBL5612427 | — | — | 1 | 6.51 |
| CHEMBL5613589 | — | — | 1 | 6.48 |
| CHEMBL5612455 | — | — | 1 | 6.47 |
| CHEMBL5614180 | — | — | 1 | 6.47 |
| CHEMBL5612876 | — | — | 1 | 6.46 |
| CHEMBL5613603 | — | — | 1 | 6.43 |
| CHEMBL5614143 | — | — | 1 | 6.43 |
| CHEMBL5613435 | — | — | 1 | 6.35 |
| CHEMBL5613854 | — | — | 1 | 6.26 |
| CHEMBL5613795 | — | — | 1 | 6.23 |
| CHEMBL5612679 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613388 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5612974 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5612649 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5612194 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5612080 | — | EC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5612003 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5613307 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5612737 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL5614206 | — | EC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5612909 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4105630 | ZURANOLONE | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL5613759 | — | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5612996 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5612666 | — | EC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5613513 | — | EC50 | = | 182.0 | nM | 6.74 |
| CHEMBL5612380 | — | EC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5613780 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5614044 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5612574 | — | EC50 | = | 241.0 | nM | 6.62 |
| CHEMBL5612427 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5613589 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5612455 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5614180 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5612876 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL5613603 | — | EC50 | = | 368.0 | nM | 6.43 |
| CHEMBL5614143 | — | EC50 | = | 371.0 | nM | 6.43 |
| CHEMBL5613435 | — | EC50 | = | 444.0 | nM | 6.35 |
| CHEMBL5613854 | — | EC50 | = | 548.0 | nM | 6.26 |
| CHEMBL5613795 | — | EC50 | = | 585.0 | nM | 6.23 |
| CHEMBL5612679 | — | EC50 | = | 784.0 | nM | 6.11 |