Assay Detail
Binding
CHEMBL713202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 1S,3R-ACPD (10 uM) -stimulated GTP gamma 35S binding on rat Metabotropic glutamate receptor 2 transfected in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.57 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290416 | — | — | 1 | 6.00 |
| CHEMBL41242 | — | — | 1 | 6.00 |
| CHEMBL38729 | — | — | 1 | 5.82 |
| CHEMBL41808 | — | — | 1 | 5.70 |
| CHEMBL288902 | — | — | 1 | 5.70 |
| CHEMBL41513 | — | — | 1 | 5.70 |
| CHEMBL289394 | — | — | 1 | 5.62 |
| CHEMBL435174 | — | — | 1 | 5.52 |
| CHEMBL41932 | — | — | 1 | 5.50 |
| CHEMBL291017 | — | — | 1 | 5.40 |
| CHEMBL439925 | — | — | 1 | 5.40 |
| CHEMBL289388 | — | — | 1 | 5.40 |
| CHEMBL290509 | — | — | 1 | 5.16 |
| CHEMBL288472 | — | — | 1 | 5.10 |
| CHEMBL38533 | — | — | 1 | - |
| CHEMBL41630 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290416 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL41242 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL38729 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL41808 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL288902 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL41513 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL289394 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL435174 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL41932 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL291017 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL439925 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL289388 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL290509 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL288472 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL38533 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL41630 | — | Ki | > | 10000.0 | nM | - |