Assay Detail
Binding
CHEMBL679479
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Displacement of [3H]baclofen from gamma-aminobutyric-acid B receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biochemical evaluation of baclofen analogues locked in the baclofen solid-state conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.67 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL701 | BACLOFEN | 4.0 | 1 | 6.38 |
| CHEMBL538722 | — | — | 1 | 4.96 |
| CHEMBL544218 | — | — | 1 | - |
| CHEMBL545618 | — | — | 1 | - |
| CHEMBL541273 | — | — | 1 | - |
| CHEMBL543270 | — | — | 1 | - |
| CHEMBL553809 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL701 | BACLOFEN | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL538722 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL544218 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL545618 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL541273 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL543270 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL553809 | — | IC50 | > | 100000.0 | nM | - |