Assay Detail
Binding
CHEMBL824294
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| Ki | 30 | 7.31 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10483 | — | — | 1 | 8.92 |
| CHEMBL49141 | — | — | 1 | 8.92 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.60 |
| CHEMBL10534 | — | — | 1 | 8.55 |
| CHEMBL1518572 | — | — | 1 | 8.38 |
| CHEMBL11709 | — | — | 1 | 8.31 |
| CHEMBL17468 | — | — | 1 | 8.08 |
| CHEMBL454095 | ABECARNIL | 2.0 | 1 | 7.82 |
| CHEMBL307783 | — | — | 1 | 7.82 |
| CHEMBL85861 | — | — | 1 | 7.73 |
| CHEMBL52750 | — | — | 1 | 7.28 |
| CHEMBL273464 | — | — | 1 | 7.11 |
| CHEMBL83464 | — | — | 1 | 7.08 |
| CHEMBL1269093 | — | — | 1 | 6.91 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.81 |
| CHEMBL66902 | — | — | 1 | 6.71 |
| CHEMBL83581 | — | — | 1 | 6.67 |
| CHEMBL87437 | — | — | 1 | 6.54 |
| CHEMBL84921 | — | — | 1 | 6.27 |
| CHEMBL86231 | — | — | 1 | 6.09 |
| CHEMBL13662 | CI-218872 | — | 1 | 5.71 |
| CHEMBL314788 | — | — | 1 | 4.53 |
| CHEMBL87331 | — | — | 1 | - |
| CHEMBL314804 | — | — | 1 | - |
| CHEMBL87641 | — | — | 1 | - |
| CHEMBL84842 | — | — | 1 | - |
| CHEMBL85539 | — | — | 1 | - |
| CHEMBL314844 | — | — | 1 | - |
| CHEMBL67421 | — | — | 1 | - |
| CHEMBL84668 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10483 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL49141 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL10534 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1518572 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL11709 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL17468 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL454095 | ABECARNIL | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL307783 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL85861 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL52750 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL273464 | — | Ki | = | 78.3 | nM | 7.11 |
| CHEMBL83464 | — | Ki | = | 82.6 | nM | 7.08 |
| CHEMBL1269093 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL66902 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL83581 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL87437 | — | Ki | = | 291.0 | nM | 6.54 |
| CHEMBL84921 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL86231 | — | Ki | = | 818.0 | nM | 6.09 |
| CHEMBL13662 | CI-218872 | Ki | = | 1964.0 | nM | 5.71 |
| CHEMBL314788 | — | Ki | = | 29700.0 | nM | 4.53 |
| CHEMBL87331 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL314804 | — | Ki | > | 300.0 | nM | - |
| CHEMBL87641 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL84842 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL85539 | — | Ki | > | 300.0 | nM | - |
| CHEMBL314844 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL67421 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL84668 | — | Ki | > | 3000.0 | nM | - |