Assay Detail
Binding
CHEMBL680688
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In vitro binding affinity to the Gamma-aminobutyric acid A receptor complex in presence of GABA in rat cerebellum tissue
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
gamma-Aminobutyrate-A receptor modulation by 3-aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.91 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79029 | — | — | 1 | 7.10 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.10 |
| CHEMBL1256760 | — | — | 1 | 7.05 |
| CHEMBL79273 | — | — | 1 | 6.68 |
| CHEMBL82083 | — | — | 1 | 6.30 |
| CHEMBL76367 | — | — | 1 | 6.14 |
| CHEMBL311213 | — | — | 1 | 6.11 |
| CHEMBL309204 | — | — | 1 | 6.05 |
| CHEMBL78307 | — | — | 1 | 5.98 |
| CHEMBL79238 | — | — | 1 | 5.96 |
| CHEMBL311927 | — | — | 1 | 5.96 |
| CHEMBL78599 | — | — | 1 | 5.85 |
| CHEMBL76738 | — | — | 1 | 5.75 |
| CHEMBL80518 | — | — | 1 | 5.66 |
| CHEMBL78461 | — | — | 1 | 5.20 |
| CHEMBL78483 | — | — | 1 | 5.19 |
| CHEMBL79231 | — | — | 1 | 5.18 |
| CHEMBL82195 | — | — | 1 | 5.00 |
| CHEMBL82476 | — | — | 1 | 5.00 |
| CHEMBL312660 | — | — | 1 | 5.00 |
| CHEMBL78422 | — | — | 1 | - |
| CHEMBL79093 | — | — | 1 | - |
| CHEMBL312265 | — | — | 1 | - |
| CHEMBL78695 | — | — | 1 | - |
| CHEMBL79384 | — | — | 1 | - |
| CHEMBL80685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79029 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1256760 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL79273 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL82083 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL76367 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL311213 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL309204 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL78307 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL79238 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL311927 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL78599 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL76738 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL80518 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL78461 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL78483 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL79231 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL82195 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL82476 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL312660 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL78422 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL79093 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL312265 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL78695 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL79384 | — | IC50 | > | 11000.0 | nM | - |
| CHEMBL80685 | — | IC50 | > | 11000.0 | nM | - |