Assay Detail
Binding
CHEMBL679644
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Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor.
18
Total Activities
17
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
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.66 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.40 |
| CHEMBL701 | BACLOFEN | 4.0 | 2 | 6.75 |
| CHEMBL87482 | 4-AMINO-3- (5-CHLOROTHIEN-2-YL)BUTANOIC ACID | — | 1 | 6.21 |
| CHEMBL83245 | — | — | 1 | 6.10 |
| CHEMBL301492 | — | — | 1 | 5.88 |
| CHEMBL86144 | — | — | 1 | 5.87 |
| CHEMBL314177 | — | — | 1 | 5.73 |
| CHEMBL315476 | — | — | 1 | 5.01 |
| CHEMBL315789 | — | — | 1 | 4.70 |
| CHEMBL87856 | — | — | 1 | 4.68 |
| CHEMBL315950 | — | — | 1 | 4.41 |
| CHEMBL85948 | — | — | 1 | 4.34 |
| CHEMBL83011 | — | — | 1 | - |
| CHEMBL85880 | — | — | 1 | - |
| CHEMBL53073 | — | — | 1 | - |
| CHEMBL315440 | — | — | 1 | - |
| CHEMBL313323 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL701 | BACLOFEN | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL701 | BACLOFEN | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL87482 | 4-AMINO-3- (5-CHLOROTHIEN-2-YL)BUTANOIC ACID | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL83245 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL301492 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL86144 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL314177 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL315476 | — | IC50 | = | 9720.0 | nM | 5.01 |
| CHEMBL315789 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL87856 | — | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL315950 | — | IC50 | = | 39100.0 | nM | 4.41 |
| CHEMBL85948 | — | IC50 | = | 45300.0 | nM | 4.34 |
| CHEMBL83011 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL85880 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53073 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL315440 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL313323 | — | IC50 | = | 124000.0 | nM | - |