Assay Detail
Binding
CHEMBL685337
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Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2
31
Total Activities
31
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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 31 | 7.27 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17468 | — | — | 1 | 9.00 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.68 |
| CHEMBL49141 | — | — | 1 | 8.62 |
| CHEMBL85861 | — | — | 1 | 8.48 |
| CHEMBL10483 | — | — | 1 | 8.40 |
| CHEMBL1518572 | — | — | 1 | 8.35 |
| CHEMBL454095 | ABECARNIL | 2.0 | 1 | 8.22 |
| CHEMBL10534 | — | — | 1 | 7.98 |
| CHEMBL11709 | — | — | 1 | 7.57 |
| CHEMBL273464 | — | — | 1 | 7.17 |
| CHEMBL307783 | — | — | 1 | 6.96 |
| CHEMBL83464 | — | — | 1 | 6.80 |
| CHEMBL87437 | — | — | 1 | 6.57 |
| CHEMBL87538 | — | — | 1 | 6.49 |
| CHEMBL83581 | — | — | 1 | 6.48 |
| CHEMBL84921 | — | — | 1 | 6.42 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.25 |
| CHEMBL52750 | — | — | 1 | 6.23 |
| CHEMBL299250 | — | — | 1 | 6.06 |
| CHEMBL66902 | — | — | 1 | 6.00 |
| CHEMBL1269093 | — | — | 1 | 6.00 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | - |
| CHEMBL87641 | — | — | 1 | - |
| CHEMBL87331 | — | — | 1 | - |
| CHEMBL86231 | — | — | 1 | - |
| CHEMBL84842 | — | — | 1 | - |
| CHEMBL314804 | — | — | 1 | - |
| CHEMBL314844 | — | — | 1 | - |
| CHEMBL85539 | — | — | 1 | - |
| CHEMBL67421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17468 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL49141 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL85861 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL10483 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1518572 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL454095 | ABECARNIL | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL10534 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL11709 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL273464 | — | Ki | = | 67.3 | nM | 7.17 |
| CHEMBL307783 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL83464 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL87437 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL87538 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL83581 | — | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL84921 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL13662 | CI-218872 | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL52750 | — | Ki | = | 591.0 | nM | 6.23 |
| CHEMBL299250 | — | Ki | = | 868.0 | nM | 6.06 |
| CHEMBL66902 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1269093 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL911 | ZOLPIDEM | Ki | > | 10000.0 | nM | - |
| CHEMBL87641 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL87331 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL86231 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL84842 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL314804 | — | Ki | > | 300.0 | nM | - |
| CHEMBL314844 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL85539 | — | Ki | > | 300.0 | nM | - |
| CHEMBL67421 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL84668 | — | Ki | > | 3000.0 | nM | - |