Assay Detail
Functional
CHEMBL680372
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro glycine reuptake inhibitory activity against glycine transporter type-2 (GlyT-2) transporter cells after incubation at 30 degrees for 30 min in presence of 50 nM [3H]glycine.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium- and chloride-dependent glycine transporter 2 (CHEMBL3195) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
5,5-Diaryl-2-amino-4-pentenoates as novel, potent, and selective glycine transporter type-2 reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.90 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28578 | — | — | 1 | 6.82 |
| CHEMBL29608 | — | — | 1 | 6.55 |
| CHEMBL29220 | — | — | 1 | 6.54 |
| CHEMBL28746 | — | — | 1 | 6.48 |
| CHEMBL30144 | — | — | 1 | 6.44 |
| CHEMBL29958 | — | — | 1 | 6.40 |
| CHEMBL28601 | — | — | 1 | 6.34 |
| CHEMBL418388 | — | — | 1 | 6.18 |
| CHEMBL28577 | — | — | 1 | 6.11 |
| CHEMBL285370 | — | — | 1 | 5.99 |
| CHEMBL29964 | — | — | 1 | 5.94 |
| CHEMBL29023 | — | — | 1 | 5.93 |
| CHEMBL27914 | — | — | 1 | 5.87 |
| CHEMBL28549 | — | — | 1 | 5.80 |
| CHEMBL283230 | — | — | 1 | 5.76 |
| CHEMBL29279 | — | — | 1 | 5.69 |
| CHEMBL281450 | — | — | 1 | 5.69 |
| CHEMBL283017 | — | — | 1 | 5.69 |
| CHEMBL27850 | — | — | 1 | 5.62 |
| CHEMBL285592 | — | — | 1 | 5.58 |
| CHEMBL29022 | — | — | 1 | 5.56 |
| CHEMBL29396 | — | — | 1 | 5.44 |
| CHEMBL286706 | — | — | 1 | 5.26 |
| CHEMBL28570 | — | — | 1 | 5.23 |
| CHEMBL28016 | — | — | 1 | 5.23 |
| CHEMBL29256 | — | — | 1 | 5.19 |
| CHEMBL416203 | — | — | 1 | - |
| CHEMBL1159913 | — | — | 1 | - |
| CHEMBL287626 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28578 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL29608 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL29220 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL28746 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL30144 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL29958 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL28601 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL418388 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL28577 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL285370 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL29964 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL29023 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL27914 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL28549 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL283230 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL29279 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL281450 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL283017 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL27850 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL285592 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL29022 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL29396 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL286706 | — | IC50 | = | 5470.0 | nM | 5.26 |
| CHEMBL28570 | — | IC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL28016 | — | IC50 | = | 5880.0 | nM | 5.23 |
| CHEMBL29256 | — | IC50 | = | 6440.0 | nM | 5.19 |
| CHEMBL416203 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1159913 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL287626 | — | IC50 | > | 10000.0 | nM | - |