Assay Detail
Binding
CHEMBL650071
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Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain cortical membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.33 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10483 | — | — | 1 | 9.00 |
| CHEMBL1518572 | — | — | 1 | 9.00 |
| CHEMBL49141 | — | — | 1 | 8.09 |
| CHEMBL87437 | — | — | 1 | 7.86 |
| CHEMBL273464 | — | — | 1 | 7.66 |
| CHEMBL85068 | — | — | 1 | 7.61 |
| CHEMBL82736 | — | — | 1 | 7.51 |
| CHEMBL83464 | — | — | 1 | 7.40 |
| CHEMBL83581 | — | — | 1 | 7.37 |
| CHEMBL87538 | — | — | 1 | 7.26 |
| CHEMBL440880 | — | — | 1 | 7.20 |
| CHEMBL84757 | — | — | 1 | 6.75 |
| CHEMBL85808 | — | — | 1 | 6.57 |
| CHEMBL420044 | — | — | 1 | 6.54 |
| CHEMBL84668 | — | — | 1 | 6.48 |
| CHEMBL84921 | — | — | 1 | 6.16 |
| CHEMBL87743 | — | — | 1 | 6.14 |
| CHEMBL85716 | — | — | 1 | - |
| CHEMBL10701 | — | — | 1 | - |
| CHEMBL314788 | — | — | 1 | - |
| CHEMBL84842 | — | — | 1 | - |
| CHEMBL87640 | — | — | 1 | - |
| CHEMBL10638 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10483 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1518572 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL49141 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL87437 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL273464 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL85068 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL82736 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL83464 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL83581 | — | IC50 | = | 43.2 | nM | 7.37 |
| CHEMBL87538 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL440880 | — | IC50 | = | 63.8 | nM | 7.20 |
| CHEMBL84757 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL85808 | — | IC50 | = | 271.4 | nM | 6.57 |
| CHEMBL420044 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL84668 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL84921 | — | IC50 | = | 697.0 | nM | 6.16 |
| CHEMBL87743 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL85716 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL10701 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL314788 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL84842 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL87640 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL10638 | — | IC50 | > | 5000.0 | nM | - |