Assay Detail
Binding
CHEMBL680656
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Binding affinity, determined by its ability to displace the [3H]GABA from Gamma-aminobutyric acid A (GABA-A) receptor site of rat brain membranes
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| 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 |
|---|---|---|---|
| Ki | 44 | 5.22 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL61683 | — | — | 1 | 7.33 |
| CHEMBL303580 | GABAZINE BROMIDE | — | 1 | 6.82 |
| CHEMBL3559482 | — | — | 1 | 6.55 |
| CHEMBL1202191 | — | — | 1 | 6.51 |
| CHEMBL1202345 | — | — | 1 | 6.37 |
| CHEMBL3559483 | — | — | 1 | 6.35 |
| CHEMBL1202188 | — | — | 1 | 6.26 |
| CHEMBL3559486 | — | — | 1 | 6.25 |
| CHEMBL1202181 | — | — | 1 | 6.24 |
| CHEMBL1202192 | — | — | 1 | 5.91 |
| CHEMBL3559481 | — | — | 1 | 5.90 |
| CHEMBL1202193 | — | — | 1 | 5.86 |
| CHEMBL609952 | — | — | 1 | 5.86 |
| CHEMBL3559484 | — | — | 1 | 5.67 |
| CHEMBL1202348 | FAMIRAPRINIUM CHLORIDE | 2.0 | 1 | 5.64 |
| CHEMBL1202347 | — | — | 1 | 5.62 |
| CHEMBL3559480 | — | — | 1 | 5.58 |
| CHEMBL1202182 | — | — | 1 | 5.43 |
| CHEMBL1202187 | — | — | 1 | 5.16 |
| CHEMBL1202195 | — | — | 1 | 5.16 |
| CHEMBL1202186 | — | — | 1 | 5.05 |
| CHEMBL1202346 | — | — | 1 | 5.00 |
| CHEMBL1202190 | — | — | 1 | 4.98 |
| CHEMBL1202183 | — | — | 1 | 4.97 |
| CHEMBL1202197 | — | — | 1 | 4.90 |
| CHEMBL1202196 | — | — | 1 | 4.70 |
| CHEMBL1202194 | — | — | 1 | 4.65 |
| CHEMBL1204018 | — | — | 1 | 4.64 |
| CHEMBL1202184 | — | — | 1 | 4.50 |
| CHEMBL556604 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL61683 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL303580 | GABAZINE BROMIDE | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3559482 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1202191 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL1202345 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL3559483 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL1202188 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL3559486 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL1202181 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL1202192 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL3559481 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL609952 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL1202193 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL3559484 | — | Ki | = | 2140.0 | nM | 5.67 |
| CHEMBL1202348 | FAMIRAPRINIUM CHLORIDE | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL1202347 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL3559480 | — | Ki | = | 2640.0 | nM | 5.58 |
| CHEMBL1202182 | — | Ki | = | 3740.0 | nM | 5.43 |
| CHEMBL1202187 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL1202195 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL1202186 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL1202346 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL1202190 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL1202183 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL1202197 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL1202196 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL1202194 | — | Ki | = | 22300.0 | nM | 4.65 |
| CHEMBL1204018 | — | Ki | = | 22800.0 | nM | 4.64 |
| CHEMBL1202184 | — | Ki | = | 31900.0 | nM | 4.50 |
| CHEMBL556604 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL292757 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL84535 | — | Ki | = | 62000.0 | nM | 4.21 |
| CHEMBL3559485 | — | Ki | = | 91200.0 | nM | 4.04 |
| CHEMBL1202189 | — | Ki | = | 91000.0 | nM | 4.04 |
| CHEMBL309739 | — | Ki | = | 91000.0 | nM | 4.04 |
| CHEMBL1202185 | — | Ki | = | 91000.0 | nM | 4.04 |
| CHEMBL439580 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL83337 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL1202840 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL310895 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL1202839 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1202198 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL431026 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1202838 | — | Ki | > | 100000.0 | nM | - |