Assay Detail
Binding
CHEMBL1273617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-3-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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 6.95 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1269816 | — | — | 1 | 8.25 |
| CHEMBL11709 | — | — | 1 | 8.24 |
| CHEMBL1270540 | — | — | 1 | 7.83 |
| CHEMBL307783 | — | — | 1 | 7.72 |
| CHEMBL1270539 | — | — | 1 | 7.61 |
| CHEMBL1270248 | — | — | 1 | 7.56 |
| CHEMBL299250 | — | — | 1 | 7.55 |
| CHEMBL1270638 | — | — | 1 | 7.50 |
| CHEMBL1269786 | — | — | 1 | 7.47 |
| CHEMBL1270037 | — | — | 1 | 7.44 |
| CHEMBL1269058 | — | — | 1 | 7.40 |
| CHEMBL1270637 | — | — | 1 | 7.38 |
| CHEMBL1269929 | — | — | 1 | 7.37 |
| CHEMBL1270639 | — | — | 1 | 7.37 |
| CHEMBL1269149 | — | — | 1 | 7.37 |
| CHEMBL1270741 | — | — | 1 | 7.35 |
| CHEMBL1270443 | — | — | 1 | 7.35 |
| CHEMBL1270144 | — | — | 1 | 7.33 |
| CHEMBL52750 | — | — | 1 | 7.16 |
| CHEMBL1270442 | — | — | 1 | 7.14 |
| CHEMBL1269148 | — | — | 1 | 7.06 |
| CHEMBL1270143 | — | — | 1 | 7.06 |
| CHEMBL1269059 | — | — | 1 | 7.00 |
| CHEMBL1269785 | — | — | 1 | 7.00 |
| CHEMBL1270038 | — | — | 1 | 6.99 |
| CHEMBL1269061 | — | — | 1 | 6.94 |
| CHEMBL1270347 | — | — | 1 | 6.93 |
| CHEMBL1269930 | — | — | 1 | 6.91 |
| CHEMBL1270538 | — | — | 1 | 6.90 |
| CHEMBL1270247 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1269816 | — | Ki | = | 5.58 | nM | 8.25 |
| CHEMBL11709 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL1270540 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL307783 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL1270539 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL1270248 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL299250 | — | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL1270638 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1269786 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL1270037 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL1269058 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL1270637 | — | Ki | = | 41.7 | nM | 7.38 |
| CHEMBL1269929 | — | Ki | = | 42.7 | nM | 7.37 |
| CHEMBL1269149 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL1270639 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL1270741 | — | Ki | = | 44.8 | nM | 7.35 |
| CHEMBL1270443 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL1270144 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL52750 | — | Ki | = | 68.8 | nM | 7.16 |
| CHEMBL1270442 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL1269148 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL1270143 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL1269785 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1269059 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1270038 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL1269061 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL1270347 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL1269930 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL1270538 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL1270247 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL1269093 | — | Ki | = | 139.2 | nM | 6.86 |
| CHEMBL1270843 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL66902 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL1270348 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL1270943 | — | Ki | = | 453.0 | nM | 6.34 |
| CHEMBL1269094 | — | Ki | = | 859.0 | nM | 6.07 |
| CHEMBL1270740 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1270841 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL13662 | CI-218872 | Ki | = | 1161.0 | nM | 5.93 |
| CHEMBL1270739 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL87641 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL87331 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL1269060 | — | Ki | = | 3942.0 | nM | 5.40 |
| CHEMBL1270944 | — | Ki | - | — | - | |
| CHEMBL1271046 | — | Ki | - | — | - |