Assay Detail
Binding
CHEMBL679478
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Antagonistic activity was measured by the inhibition of Gamma-aminobutyric acid type B receptor binding to rat brain synaptosomes
16
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Substituted morpholine-2S-acetic acid derivatives: Sch 50911 and related compounds as novel GABAB antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.94 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2093975 | — | — | 1 | 5.96 |
| CHEMBL544240 | — | — | 2 | 5.70 |
| CHEMBL543293 | — | — | 2 | 5.52 |
| CHEMBL542594 | — | — | 2 | 5.05 |
| CHEMBL2093976 | — | — | 1 | 5.00 |
| CHEMBL541037 | — | — | 1 | 4.96 |
| CHEMBL554872 | — | — | 2 | 4.72 |
| CHEMBL544716 | — | — | 1 | 4.43 |
| CHEMBL40157 | — | — | 1 | 4.21 |
| CHEMBL3350240 | — | — | 1 | - |
| CHEMBL545408 | — | — | 1 | - |
| CHEMBL2094023 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2093975 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL544240 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL543293 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL544240 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL542594 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2093976 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL541037 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL554872 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL542594 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL544716 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL40157 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL554872 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3350240 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL545408 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2094023 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL543293 | — | IC50 | > | 100000.0 | nM | - |