Assay Detail
Binding
CHEMBL4481482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]muscimol from orthosteric binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting
40
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 6.80 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1093534 | — | — | 1 | 8.55 |
| CHEMBL1851667 | — | — | 2 | 7.81 |
| CHEMBL1091277 | — | — | 1 | 7.52 |
| CHEMBL4586160 | — | — | 2 | 7.41 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.31 |
| CHEMBL32503 | GABAZINE | — | 1 | 7.13 |
| CHEMBL4586737 | — | — | 2 | 7.11 |
| CHEMBL4589563 | — | — | 2 | 6.89 |
| CHEMBL4515872 | — | — | 2 | 6.66 |
| CHEMBL131516 | — | — | 2 | 6.23 |
| CHEMBL4543048 | — | — | 2 | 6.13 |
| CHEMBL133180 | — | — | 2 | 6.10 |
| CHEMBL4588159 | — | — | 2 | 6.07 |
| CHEMBL4570040 | — | — | 2 | 5.96 |
| CHEMBL1342 | OXYBATE | 4.0 | 1 | - |
| CHEMBL1204604 | — | — | 1 | - |
| CHEMBL4587203 | — | — | 1 | - |
| CHEMBL4553063 | — | — | 1 | - |
| CHEMBL4540258 | — | — | 1 | - |
| CHEMBL4536994 | — | — | 1 | - |
| CHEMBL4522479 | — | — | 1 | - |
| CHEMBL4571202 | — | — | 1 | - |
| CHEMBL4529526 | — | — | 1 | - |
| CHEMBL4593644 | — | — | 1 | - |
| CHEMBL4581397 | — | — | 1 | - |
| CHEMBL4519194 | — | — | 1 | - |
| CHEMBL4530576 | — | — | 1 | - |
| CHEMBL4578710 | — | — | 1 | - |
| CHEMBL4538191 | — | — | 1 | - |
| CHEMBL4566181 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1093534 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1851667 | — | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL1851667 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1091277 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4586160 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4586160 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL32503 | GABAZINE | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL4586737 | — | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL4586737 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4589563 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4589563 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL4515872 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL4515872 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL131516 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL131516 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL4543048 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL4543048 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL133180 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL133180 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL4588159 | — | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL4588159 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL4570040 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4570040 | — | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL1342 | OXYBATE | Ki | > | 1000000.0 | nM | - |
| CHEMBL1204604 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4587203 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4553063 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4540258 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4536994 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4571202 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4529526 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4593644 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4581397 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4519194 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4530576 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4578710 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4566181 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4538191 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4522479 | — | Ki | > | 100000.0 | nM | - |