Assay Detail
Binding
CHEMBL679643
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In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Publication
Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.75 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112710 | — | — | 1 | 9.00 |
| CHEMBL112203 | — | — | 1 | 8.52 |
| CHEMBL701 | BACLOFEN | 4.0 | 1 | 7.52 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.22 |
| CHEMBL113571 | — | — | 1 | 6.00 |
| CHEMBL149082 | TRAMIPROSATE | 3.0 | 1 | 5.70 |
| CHEMBL286077 | — | — | 1 | 5.70 |
| CHEMBL40157 | — | — | 1 | 5.60 |
| CHEMBL325921 | — | — | 1 | 5.52 |
| CHEMBL341858 | — | — | 1 | - |
| CHEMBL146972 | PHOSPHORYLETHANOLAMINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112710 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL112203 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL701 | BACLOFEN | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL113571 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL149082 | TRAMIPROSATE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL286077 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL40157 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL325921 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL341858 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL146972 | PHOSPHORYLETHANOLAMINE | IC50 | > | 100000.0 | nM | - |