Assay Detail
Binding
CHEMBL4429876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of glycine transporter-1B in human JAR cells assessed as reduction in [14C]glycine uptake preincubated for 10 mins followed by [14C]glycine addition measured after 3 hrs by scintillation proximity assay
35
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | JAR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent glycine transporter 1 (CHEMBL2337) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.86 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593786 | — | — | 1 | 9.17 |
| CHEMBL4526580 | — | — | 1 | 9.14 |
| CHEMBL4468117 | — | — | 1 | 9.13 |
| CHEMBL4448986 | — | — | 3 | 8.99 |
| CHEMBL4456392 | — | — | 1 | 8.94 |
| CHEMBL4582587 | — | — | 1 | 8.91 |
| CHEMBL4516089 | — | — | 1 | 8.90 |
| CHEMBL4572086 | — | — | 1 | 8.83 |
| CHEMBL4579165 | — | — | 1 | 8.81 |
| CHEMBL4462009 | — | — | 1 | 8.67 |
| CHEMBL4532784 | — | — | 1 | 8.63 |
| CHEMBL4573115 | — | — | 1 | 8.29 |
| CHEMBL4555741 | — | — | 1 | 8.29 |
| CHEMBL4439865 | — | — | 1 | 8.28 |
| CHEMBL4475426 | — | — | 1 | 8.26 |
| CHEMBL4447922 | — | — | 1 | 8.08 |
| CHEMBL4458568 | — | — | 1 | 7.90 |
| CHEMBL4579970 | — | — | 1 | 7.82 |
| CHEMBL4450109 | — | — | 1 | 7.74 |
| CHEMBL4565929 | — | — | 1 | 7.64 |
| CHEMBL4455289 | — | — | 1 | 7.54 |
| CHEMBL4451800 | — | — | 1 | 7.54 |
| CHEMBL4455686 | — | — | 1 | 7.44 |
| CHEMBL4533944 | — | — | 1 | 7.42 |
| CHEMBL4550823 | — | — | 1 | 7.37 |
| CHEMBL4536223 | — | — | 1 | 7.25 |
| CHEMBL4580509 | — | — | 1 | 7.13 |
| CHEMBL4590387 | — | — | 1 | 6.84 |
| CHEMBL4462786 | — | — | 1 | 6.50 |
| CHEMBL4581616 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593786 | — | IC50 | = | 0.671 | nM | 9.17 |
| CHEMBL4526580 | — | IC50 | = | 0.726 | nM | 9.14 |
| CHEMBL4468117 | — | IC50 | = | 0.733 | nM | 9.13 |
| CHEMBL4448986 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL4448986 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL4456392 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL4582587 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL4516089 | — | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL4572086 | — | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL4579165 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL4462009 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL4532784 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL4573115 | — | IC50 | = | 5.09 | nM | 8.29 |
| CHEMBL4555741 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4439865 | — | IC50 | = | 5.29 | nM | 8.28 |
| CHEMBL4475426 | — | IC50 | = | 5.56 | nM | 8.26 |
| CHEMBL4447922 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4458568 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4579970 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL4450109 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL4565929 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL4451800 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4455289 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL4448986 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL4455686 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL4533944 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL4550823 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL4536223 | — | IC50 | = | 56.6 | nM | 7.25 |
| CHEMBL4580509 | — | IC50 | = | 73.8 | nM | 7.13 |
| CHEMBL4590387 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4462786 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4581616 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL4548066 | — | IC50 | = | 952.0 | nM | 6.02 |
| CHEMBL4583686 | — | IC50 | = | 2294.0 | nM | 5.64 |
| CHEMBL4578210 | — | IC50 | = | 9363.0 | nM | 5.03 |