Assay Detail
Binding
CHEMBL679653
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Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.06 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.52 |
| CHEMBL701 | BACLOFEN | 4.0 | 1 | 6.70 |
| CHEMBL162716 | — | — | 1 | 5.25 |
| CHEMBL349520 | — | — | 1 | 4.75 |
| CHEMBL536701 | — | — | 1 | - |
| CHEMBL543481 | — | — | 1 | - |
| CHEMBL164731 | — | — | 1 | - |
| CHEMBL162149 | — | — | 1 | - |
| CHEMBL542038 | — | — | 1 | - |
| CHEMBL315440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL701 | BACLOFEN | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL162716 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL349520 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL536701 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL543481 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL164731 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL162149 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL542038 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL315440 | — | IC50 | > | 100000.0 | nM | - |