Assay Detail
Binding
CHEMBL686133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]GABA binding to Gamma-aminobutyric acid A (GABA-A) receptor of rat brain membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of gamma-aminobutyric acid acting as selective GABA-A antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.14 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 1 | 6.05 |
| CHEMBL20489 | OMPENACLID | 2.0 | 1 | 5.75 |
| CHEMBL281593 | GUANIDINO ACETATE | — | 1 | 5.68 |
| CHEMBL309378 | — | — | 1 | 5.05 |
| CHEMBL83666 | — | — | 1 | 4.75 |
| CHEMBL20443 | — | — | 1 | 4.54 |
| CHEMBL419113 | — | — | 1 | 4.17 |
| CHEMBL84253 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL784 | IMIDAZOLE ACETIC ACID | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL20489 | OMPENACLID | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL281593 | GUANIDINO ACETATE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL309378 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL83666 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL20443 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL419113 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL84253 | — | IC50 | = | 290000.0 | nM | - |