Assay Detail
Binding
CHEMBL822162
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Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor
32
Total Activities
32
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 32 | 7.78 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10483 | — | — | 1 | 9.85 |
| CHEMBL49141 | — | — | 1 | 9.31 |
| CHEMBL10534 | — | — | 1 | 9.22 |
| CHEMBL307783 | — | — | 1 | 9.14 |
| CHEMBL11709 | — | — | 1 | 8.92 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.66 |
| CHEMBL1518572 | — | — | 1 | 8.39 |
| CHEMBL52750 | — | — | 1 | 8.28 |
| CHEMBL17468 | — | — | 1 | 8.24 |
| CHEMBL85861 | — | — | 1 | 8.21 |
| CHEMBL299250 | — | — | 1 | 8.19 |
| CHEMBL454095 | ABECARNIL | 2.0 | 1 | 7.91 |
| CHEMBL87538 | — | — | 1 | 7.81 |
| CHEMBL273464 | — | — | 1 | 7.68 |
| CHEMBL83581 | — | — | 1 | 7.61 |
| CHEMBL83464 | — | — | 1 | 7.60 |
| CHEMBL1269093 | — | — | 1 | 7.60 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.57 |
| CHEMBL66902 | — | — | 1 | 7.43 |
| CHEMBL84921 | — | — | 1 | 7.35 |
| CHEMBL13662 | CI-218872 | — | 1 | 7.24 |
| CHEMBL87437 | — | — | 1 | 6.74 |
| CHEMBL86231 | — | — | 1 | 6.61 |
| CHEMBL67421 | — | — | 1 | 6.55 |
| CHEMBL87641 | — | — | 1 | 6.46 |
| CHEMBL87331 | — | — | 1 | 6.08 |
| CHEMBL314788 | — | — | 1 | 5.44 |
| CHEMBL314804 | — | — | 1 | - |
| CHEMBL85539 | — | — | 1 | - |
| CHEMBL84842 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10483 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL49141 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL10534 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL307783 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL11709 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1518572 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL52750 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL17468 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL85861 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL299250 | — | Ki | = | 6.43 | nM | 8.19 |
| CHEMBL454095 | ABECARNIL | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL87538 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL273464 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL83581 | — | Ki | = | 24.6 | nM | 7.61 |
| CHEMBL1269093 | — | Ki | = | 24.9 | nM | 7.60 |
| CHEMBL83464 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL66902 | — | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL84921 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL13662 | CI-218872 | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL87437 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL86231 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL67421 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL87641 | — | Ki | = | 350.2 | nM | 6.46 |
| CHEMBL87331 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL314788 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL314804 | — | Ki | > | 300.0 | nM | - |
| CHEMBL85539 | — | Ki | > | 300.0 | nM | - |
| CHEMBL84842 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL314844 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL84668 | — | Ki | > | 1000.0 | nM | - |