Assay Detail
Binding
CHEMBL1273615
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 7.74 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307783 | — | — | 1 | 9.14 |
| CHEMBL1270038 | — | — | 1 | 9.01 |
| CHEMBL11709 | — | — | 1 | 8.92 |
| CHEMBL1270540 | — | — | 1 | 8.79 |
| CHEMBL1270248 | — | — | 1 | 8.62 |
| CHEMBL1270539 | — | — | 1 | 8.56 |
| CHEMBL1270637 | — | — | 1 | 8.52 |
| CHEMBL1270443 | — | — | 1 | 8.44 |
| CHEMBL1269058 | — | — | 1 | 8.43 |
| CHEMBL1270638 | — | — | 1 | 8.40 |
| CHEMBL1269816 | — | — | 1 | 8.36 |
| CHEMBL1269929 | — | — | 1 | 8.35 |
| CHEMBL1269786 | — | — | 1 | 8.32 |
| CHEMBL52750 | — | — | 1 | 8.28 |
| CHEMBL299250 | — | — | 1 | 8.19 |
| CHEMBL1270037 | — | — | 1 | 8.17 |
| CHEMBL1269149 | — | — | 1 | 8.11 |
| CHEMBL1270442 | — | — | 1 | 8.04 |
| CHEMBL1270639 | — | — | 1 | 8.00 |
| CHEMBL1270144 | — | — | 1 | 7.92 |
| CHEMBL1269930 | — | — | 1 | 7.84 |
| CHEMBL1269148 | — | — | 1 | 7.77 |
| CHEMBL1270143 | — | — | 1 | 7.77 |
| CHEMBL1269061 | — | — | 1 | 7.75 |
| CHEMBL1270741 | — | — | 1 | 7.66 |
| CHEMBL1270538 | — | — | 1 | 7.60 |
| CHEMBL1269093 | — | — | 1 | 7.60 |
| CHEMBL1270347 | — | — | 1 | 7.58 |
| CHEMBL1270943 | — | — | 1 | 7.57 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307783 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL1270038 | — | Ki | = | 0.972 | nM | 9.01 |
| CHEMBL11709 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1270540 | — | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL1270248 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1270539 | — | Ki | = | 2.78 | nM | 8.56 |
| CHEMBL1270637 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1270443 | — | Ki | = | 3.63 | nM | 8.44 |
| CHEMBL1269058 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1270638 | — | Ki | = | 3.99 | nM | 8.40 |
| CHEMBL1269816 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1269929 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1269786 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL52750 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL299250 | — | Ki | = | 6.43 | nM | 8.19 |
| CHEMBL1270037 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL1269149 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL1270442 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL1270639 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1270144 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1269930 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL1269148 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1270143 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1269061 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1270741 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1270538 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1269093 | — | Ki | = | 24.9 | nM | 7.60 |
| CHEMBL1270347 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1270943 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL1269785 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1269059 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1270841 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL1270348 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL66902 | — | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL13662 | CI-218872 | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL1270247 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL1270843 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL1269060 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1269094 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL87641 | — | Ki | = | 350.2 | nM | 6.46 |
| CHEMBL1270944 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL87331 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL1270740 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1270739 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL1271046 | — | Ki | - | — | - |