Assay Detail
Binding
CHEMBL993724
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Inhibition of [3H]glycine uptake at human glycine transporter 1 expressed in human JAR cells after 3 hrs by scintillation counting
23
Total Activities
23
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
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.94 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485356 | — | — | 1 | 10.00 |
| CHEMBL483938 | — | — | 1 | 9.51 |
| CHEMBL521463 | — | — | 1 | 9.19 |
| CHEMBL482764 | — | — | 1 | 8.76 |
| CHEMBL482960 | — | — | 1 | 8.72 |
| CHEMBL484734 | — | — | 1 | 8.70 |
| CHEMBL483344 | — | — | 1 | 8.59 |
| CHEMBL521182 | — | — | 1 | 8.53 |
| CHEMBL485355 | — | — | 1 | 8.44 |
| CHEMBL484733 | — | — | 1 | 8.36 |
| CHEMBL483157 | — | — | 1 | 8.27 |
| CHEMBL520648 | — | — | 1 | 8.26 |
| CHEMBL482974 | — | — | 1 | 7.99 |
| CHEMBL485139 | — | — | 1 | 7.94 |
| CHEMBL483345 | — | — | 1 | 7.55 |
| CHEMBL484179 | — | — | 1 | 7.50 |
| CHEMBL482754 | — | — | 1 | 6.91 |
| CHEMBL482964 | — | — | 1 | 6.90 |
| CHEMBL485366 | — | — | 1 | 6.88 |
| CHEMBL485534 | — | — | 1 | 6.73 |
| CHEMBL482546 | — | — | 1 | 6.50 |
| CHEMBL520956 | — | — | 1 | 6.30 |
| CHEMBL519701 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485356 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL483938 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL521463 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL482764 | — | IC50 | = | 1.74 | nM | 8.76 |
| CHEMBL482960 | — | IC50 | = | 1.89 | nM | 8.72 |
| CHEMBL484734 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL483344 | — | IC50 | = | 2.58 | nM | 8.59 |
| CHEMBL521182 | — | IC50 | = | 2.95 | nM | 8.53 |
| CHEMBL485355 | — | IC50 | = | 3.62 | nM | 8.44 |
| CHEMBL484733 | — | IC50 | = | 4.33 | nM | 8.36 |
| CHEMBL483157 | — | IC50 | = | 5.43 | nM | 8.27 |
| CHEMBL520648 | — | IC50 | = | 5.44 | nM | 8.26 |
| CHEMBL482974 | — | IC50 | = | 10.35 | nM | 7.99 |
| CHEMBL485139 | — | IC50 | = | 11.55 | nM | 7.94 |
| CHEMBL483345 | — | IC50 | = | 28.22 | nM | 7.55 |
| CHEMBL484179 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL482754 | — | IC50 | = | 123.6 | nM | 6.91 |
| CHEMBL482964 | — | IC50 | = | 124.6 | nM | 6.90 |
| CHEMBL485366 | — | IC50 | = | 131.7 | nM | 6.88 |
| CHEMBL485534 | — | IC50 | = | 184.9 | nM | 6.73 |
| CHEMBL482546 | — | IC50 | = | 314.3 | nM | 6.50 |
| CHEMBL520956 | — | IC50 | = | 501.6 | nM | 6.30 |
| CHEMBL519701 | — | IC50 | = | 870.8 | nM | 6.06 |