Assay Detail
Binding
CHEMBL3423809
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Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.00 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201284 | CINACALCET | 4.0 | 1 | 6.50 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.50 |
| CHEMBL1200969 | DUTASTERIDE | 4.0 | 1 | 6.48 |
| CHEMBL15770 | SULINDAC | 4.0 | 1 | 6.42 |
| CHEMBL1042 | CHOLECALCIFEROL | 4.0 | 1 | 6.40 |
| CHEMBL46516 | FLUSPIRILENE | 3.0 | 1 | 5.92 |
| CHEMBL1265 | ADAPALENE | 4.0 | 1 | 5.89 |
| CHEMBL465 | DRONABINOL | 4.0 | 1 | 5.89 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 5.77 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 5.75 |
| CHEMBL416956 | MEFLOQUINE | 4.0 | 1 | 5.60 |
| CHEMBL1017 | TELMISARTAN | 4.0 | 1 | 5.50 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201284 | CINACALCET | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL85 | RISPERIDONE | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1200969 | DUTASTERIDE | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL15770 | SULINDAC | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL1042 | CHOLECALCIFEROL | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL46516 | FLUSPIRILENE | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1265 | ADAPALENE | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL465 | DRONABINOL | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1423 | PIMOZIDE | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1946170 | REGORAFENIB | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL416956 | MEFLOQUINE | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1017 | TELMISARTAN | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL296419 | ASTEMIZOLE | EC50 | = | 4200.0 | nM | 5.38 |