Assay Detail
Binding
CHEMBL4820883
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Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced currents by whole-cell patch-clamp assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
C-2-Linked Dimeric Strychnine Analogues as Bivalent Ligands Targeting Glycine Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.31 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227934 | STRYCHNINE | -1.0 | 1 | 7.30 |
| CHEMBL4849489 | — | — | 1 | 7.05 |
| CHEMBL4870499 | — | — | 1 | 7.00 |
| CHEMBL4857611 | — | — | 1 | 6.89 |
| CHEMBL4851242 | — | — | 1 | 6.77 |
| CHEMBL4848356 | — | — | 1 | 6.40 |
| CHEMBL4850957 | — | — | 1 | 6.14 |
| CHEMBL4860026 | — | — | 1 | 5.96 |
| CHEMBL4873219 | — | — | 1 | 5.85 |
| CHEMBL4849060 | — | — | 1 | 5.82 |
| CHEMBL4849579 | — | — | 1 | 5.77 |
| CHEMBL4861263 | — | — | 1 | 5.54 |
| CHEMBL4878671 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227934 | STRYCHNINE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4849489 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4870499 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4857611 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4851242 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4848356 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4850957 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4860026 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4873219 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4849060 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4849579 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4861263 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4878671 | — | IC50 | = | 3100.0 | nM | 5.51 |