Assay Detail
Binding
CHEMBL3430053
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant alpha1beta2gamma2 GABAA receptor (unknown origin) expressed in LTK cells assessed as potentiation of GABA-induced channel current treated for 30 s prior to GABA stimulation for 2s 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 | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; agonist GABA site (CHEMBL2109244) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.06 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3427532 | — | — | 1 | 6.90 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 6.62 |
| CHEMBL1568698 | GANAXOLONE | 4.0 | 1 | 6.58 |
| CHEMBL3427519 | — | — | 1 | 6.45 |
| CHEMBL3427528 | — | — | 1 | 6.43 |
| CHEMBL3427523 | — | — | 1 | 6.23 |
| CHEMBL3427537 | — | — | 1 | 6.14 |
| CHEMBL3427526 | — | — | 1 | 6.03 |
| CHEMBL3427530 | — | — | 1 | 6.03 |
| CHEMBL3427535 | — | — | 1 | 5.94 |
| CHEMBL3427538 | — | — | 1 | 5.83 |
| CHEMBL3427540 | — | — | 1 | 5.81 |
| CHEMBL3427542 | — | — | 1 | 5.76 |
| CHEMBL3427533 | — | — | 1 | 5.74 |
| CHEMBL3427539 | — | — | 1 | 5.72 |
| CHEMBL3427536 | — | — | 1 | 5.66 |
| CHEMBL3427548 | — | — | 1 | 5.60 |
| CHEMBL3427524 | — | — | 1 | 5.56 |
| CHEMBL3427534 | — | — | 1 | - |
| CHEMBL3427531 | — | — | 1 | - |
| CHEMBL3427527 | — | — | 1 | - |
| CHEMBL3427525 | — | — | 1 | - |
| CHEMBL3427541 | — | — | 1 | - |
| CHEMBL3427522 | — | — | 1 | - |
| CHEMBL3427543 | — | — | 1 | - |
| CHEMBL3427544 | — | — | 1 | - |
| CHEMBL3427545 | — | — | 1 | - |
| CHEMBL3427546 | — | — | 1 | - |
| CHEMBL3427547 | — | — | 1 | - |
| CHEMBL3427521 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3427532 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL207538 | BREXANOLONE | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL1568698 | GANAXOLONE | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL3427519 | — | EC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3427528 | — | EC50 | = | 371.0 | nM | 6.43 |
| CHEMBL3427523 | — | EC50 | = | 592.0 | nM | 6.23 |
| CHEMBL3427537 | — | EC50 | = | 724.0 | nM | 6.14 |
| CHEMBL3427526 | — | EC50 | = | 945.0 | nM | 6.03 |
| CHEMBL3427530 | — | EC50 | = | 945.0 | nM | 6.03 |
| CHEMBL3427535 | — | EC50 | = | 1151.0 | nM | 5.94 |
| CHEMBL3427538 | — | EC50 | = | 1491.0 | nM | 5.83 |
| CHEMBL3427540 | — | EC50 | = | 1534.0 | nM | 5.81 |
| CHEMBL3427542 | — | EC50 | = | 1749.0 | nM | 5.76 |
| CHEMBL3427533 | — | EC50 | = | 1836.0 | nM | 5.74 |
| CHEMBL3427539 | — | EC50 | = | 1902.0 | nM | 5.72 |
| CHEMBL3427536 | — | EC50 | = | 2198.0 | nM | 5.66 |
| CHEMBL3427548 | — | EC50 | = | 2515.0 | nM | 5.60 |
| CHEMBL3427524 | — | EC50 | = | 2738.0 | nM | 5.56 |
| CHEMBL3427534 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427531 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427527 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427525 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427541 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427522 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427543 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427544 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427545 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427546 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427547 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3427521 | — | EC50 | > | 3000.0 | nM | - |