Assay Detail
Binding
CHEMBL1273619
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-5-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 6.39 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1270540 | — | — | 1 | 8.34 |
| CHEMBL1270539 | — | — | 1 | 8.13 |
| CHEMBL11709 | — | — | 1 | 7.57 |
| CHEMBL1269816 | — | — | 1 | 7.33 |
| CHEMBL1269930 | — | — | 1 | 7.18 |
| CHEMBL1269149 | — | — | 1 | 7.16 |
| CHEMBL1270443 | — | — | 1 | 7.12 |
| CHEMBL1270037 | — | — | 1 | 6.97 |
| CHEMBL307783 | — | — | 1 | 6.96 |
| CHEMBL1270144 | — | — | 1 | 6.91 |
| CHEMBL1269929 | — | — | 1 | 6.91 |
| CHEMBL1270347 | — | — | 1 | 6.90 |
| CHEMBL1270637 | — | — | 1 | 6.90 |
| CHEMBL1270248 | — | — | 1 | 6.79 |
| CHEMBL1270639 | — | — | 1 | 6.72 |
| CHEMBL1270038 | — | — | 1 | 6.68 |
| CHEMBL1269061 | — | — | 1 | 6.67 |
| CHEMBL1269058 | — | — | 1 | 6.59 |
| CHEMBL1269786 | — | — | 1 | 6.54 |
| CHEMBL1270538 | — | — | 1 | 6.52 |
| CHEMBL1270741 | — | — | 1 | 6.38 |
| CHEMBL1270442 | — | — | 1 | 6.35 |
| CHEMBL1270638 | — | — | 1 | 6.34 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.25 |
| CHEMBL52750 | — | — | 1 | 6.23 |
| CHEMBL1270247 | — | — | 1 | 6.17 |
| CHEMBL299250 | — | — | 1 | 6.08 |
| CHEMBL1270740 | — | — | 1 | 6.00 |
| CHEMBL1269093 | — | — | 1 | 6.00 |
| CHEMBL1270841 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1270540 | — | Ki | = | 4.61 | nM | 8.34 |
| CHEMBL1270539 | — | Ki | = | 7.49 | nM | 8.13 |
| CHEMBL11709 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL1269816 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL1269930 | — | Ki | = | 65.3 | nM | 7.18 |
| CHEMBL1269149 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL1270443 | — | Ki | = | 76.5 | nM | 7.12 |
| CHEMBL1270037 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL307783 | — | Ki | = | 110.8 | nM | 6.96 |
| CHEMBL1270144 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1269929 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL1270347 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL1270637 | — | Ki | = | 125.7 | nM | 6.90 |
| CHEMBL1270248 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL1270639 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL1270038 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL1269061 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL1269058 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL1269786 | — | Ki | = | 286.0 | nM | 6.54 |
| CHEMBL1270538 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL1270741 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL1270442 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL1270638 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL13662 | CI-218872 | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL52750 | — | Ki | = | 591.0 | nM | 6.23 |
| CHEMBL1270247 | — | Ki | = | 681.0 | nM | 6.17 |
| CHEMBL299250 | — | Ki | = | 826.0 | nM | 6.08 |
| CHEMBL1270740 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1269093 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1270841 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL66902 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1269148 | — | Ki | = | 1444.0 | nM | 5.84 |
| CHEMBL1270143 | — | Ki | = | 1444.0 | nM | 5.84 |
| CHEMBL1271046 | — | Ki | = | 1847.0 | nM | 5.73 |
| CHEMBL1270843 | — | Ki | = | 1847.0 | nM | 5.73 |
| CHEMBL1270943 | — | Ki | = | 1847.0 | nM | 5.73 |
| CHEMBL1270739 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL1270348 | — | Ki | = | 2861.0 | nM | 5.54 |
| CHEMBL87641 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL1269060 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL1270944 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL87331 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL1269094 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL911 | ZOLPIDEM | Ki | > | 10000.0 | nM | - |
| CHEMBL1269785 | — | Ki | > | 300.0 | nM | - |
| CHEMBL1269059 | — | Ki | > | 300.0 | nM | - |