Assay Detail
Binding
CHEMBL4434264
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GlyT2 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake at pH 7.5 by scintillation spectroscopy
5
Total Activities
5
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
Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.08 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475562 | — | — | 1 | 7.58 |
| CHEMBL4439878 | — | — | 1 | 6.32 |
| CHEMBL4452842 | — | — | 1 | 6.29 |
| CHEMBL180966 | — | — | 1 | 5.75 |
| CHEMBL4566424 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475562 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4439878 | — | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4452842 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL180966 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4566424 | — | IC50 | = | 33200.0 | nM | 4.48 |