Assay Detail
Binding
CHEMBL4481260
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversible non-competitive inhibition of human GlyT2a expressed in Xenopus laevis oocytes by two-electrode voltage clamp electrophysiology
6
Total Activities
6
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 |
Target
Sodium- and chloride-dependent glycine transporter 2 (CHEMBL3060) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.67 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4531406 | — | — | 1 | 6.47 |
| CHEMBL226118 | OLEOYL GLYCINE | — | 1 | 6.30 |
| CHEMBL3392050 | — | — | 1 | 6.22 |
| CHEMBL161343 | ARACHIDONOYL GLYCINE | — | 1 | 5.05 |
| CHEMBL226400 | — | — | 1 | 5.05 |
| CHEMBL456340 | ARACHIDONOYL GABA | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4531406 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL226118 | OLEOYL GLYCINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3392050 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL161343 | ARACHIDONOYL GLYCINE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL226400 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL456340 | ARACHIDONOYL GABA | IC50 | = | 12000.0 | nM | 4.92 |