Assay Detail
Binding
CHEMBL1657779
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Inhibition of [3H]glycine uptake at GlyT1 in rat C6 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | C6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent glycine transporter 1 (CHEMBL4556) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.78 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1649969 | — | — | 1 | 7.08 |
| CHEMBL1649956 | — | — | 1 | 7.00 |
| CHEMBL1649588 | — | — | 1 | 6.72 |
| CHEMBL1649954 | — | — | 1 | 6.72 |
| CHEMBL1649974 | — | — | 1 | 6.66 |
| CHEMBL1649957 | — | — | 1 | 6.62 |
| CHEMBL1649958 | — | — | 1 | 6.52 |
| CHEMBL1649975 | — | — | 1 | 6.43 |
| CHEMBL1649955 | — | — | 1 | 6.41 |
| CHEMBL1649970 | — | — | 1 | 6.29 |
| CHEMBL1649949 | — | — | 1 | 6.06 |
| CHEMBL1649959 | — | — | 1 | 6.04 |
| CHEMBL1649971 | — | — | 1 | 6.00 |
| CHEMBL87351 | — | — | 1 | 5.75 |
| CHEMBL1649968 | — | — | 1 | 5.64 |
| CHEMBL1649976 | — | — | 1 | 5.58 |
| CHEMBL1649952 | — | — | 1 | 5.52 |
| CHEMBL1649960 | — | — | 1 | 5.42 |
| CHEMBL1649950 | — | — | 1 | 5.28 |
| CHEMBL1649972 | — | — | 1 | 5.19 |
| CHEMBL1649964 | — | — | 1 | 5.01 |
| CHEMBL1649961 | — | — | 1 | 4.96 |
| CHEMBL1649967 | — | — | 1 | 4.57 |
| CHEMBL1649951 | — | — | 1 | 4.46 |
| CHEMBL1649965 | — | — | 1 | 4.21 |
| CHEMBL1649966 | — | — | 1 | 4.16 |
| CHEMBL1649963 | — | — | 1 | - |
| CHEMBL1649962 | — | — | 1 | - |
| CHEMBL1649953 | — | — | 1 | - |
| CHEMBL1649973 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1649969 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1649956 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1649588 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1649954 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1649974 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1649957 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1649958 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1649975 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1649955 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1649970 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1649949 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1649959 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1649971 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL87351 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1649968 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1649976 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1649952 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1649960 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1649950 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL1649972 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1649964 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1649961 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1649967 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL1649951 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1649965 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL1649966 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL1649963 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1649962 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1649953 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1649973 | — | IC50 | > | 10000.0 | nM | - |