Assay Detail
Functional
CHEMBL4309033
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Positive allosteric modulation of human mGlu2 receptor expressed in CHOK1 cell membranes assessed as increase in glutamate-induced [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins by scintillation spectrometry method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.29 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4589377 | — | — | 1 | 7.82 |
| CHEMBL3947764 | — | — | 1 | 7.74 |
| CHEMBL4468977 | — | — | 1 | 6.80 |
| CHEMBL4538850 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4589377 | — | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL3947764 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL4468977 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4538850 | — | EC50 | = | 158.49 | nM | 6.80 |