Assay Detail
Functional
CHEMBL899072
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Activity at GABAB 1b/2 receptor expressed in CHO-K1 cells assessed as effect on glutamate-induced [35S]GTP-gamma-S binding
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.71 | 6.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392394 | GS-39783 | — | 1 | 6.13 |
| CHEMBL393066 | — | — | 1 | 6.06 |
| CHEMBL391647 | — | — | 1 | 5.92 |
| CHEMBL276131 | — | — | 1 | 5.78 |
| CHEMBL393269 | — | — | 1 | 5.78 |
| CHEMBL237801 | — | — | 1 | 5.78 |
| CHEMBL392365 | — | — | 1 | 5.69 |
| CHEMBL237582 | — | — | 1 | 5.56 |
| CHEMBL401437 | — | — | 1 | 5.46 |
| CHEMBL237581 | — | — | 1 | 5.34 |
| CHEMBL391576 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392394 | GS-39783 | EC50 | = | 741.31 | nM | 6.13 |
| CHEMBL393066 | — | EC50 | = | 870.96 | nM | 6.06 |
| CHEMBL391647 | — | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL276131 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL393269 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL237801 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL392365 | — | EC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL237582 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL401437 | — | EC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL237581 | — | EC50 | = | 4570.88 | nM | 5.34 |
| CHEMBL391576 | — | EC50 | = | 5011.87 | nM | 5.30 |