Assay Detail
Binding
CHEMBL1273616
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-2-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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| 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 | 7.03 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1270443 | — | — | 1 | 8.70 |
| CHEMBL1269816 | — | — | 1 | 8.35 |
| CHEMBL1270540 | — | — | 1 | 8.34 |
| CHEMBL11709 | — | — | 1 | 8.31 |
| CHEMBL1270638 | — | — | 1 | 8.10 |
| CHEMBL1270539 | — | — | 1 | 8.05 |
| CHEMBL1270442 | — | — | 1 | 7.89 |
| CHEMBL1270248 | — | — | 1 | 7.89 |
| CHEMBL307783 | — | — | 1 | 7.82 |
| CHEMBL1270637 | — | — | 1 | 7.61 |
| CHEMBL299250 | — | — | 1 | 7.60 |
| CHEMBL1269058 | — | — | 1 | 7.57 |
| CHEMBL1270037 | — | — | 1 | 7.52 |
| CHEMBL1269786 | — | — | 1 | 7.51 |
| CHEMBL1269149 | — | — | 1 | 7.49 |
| CHEMBL1270639 | — | — | 1 | 7.48 |
| CHEMBL1270144 | — | — | 1 | 7.41 |
| CHEMBL1269929 | — | — | 1 | 7.35 |
| CHEMBL1269930 | — | — | 1 | 7.35 |
| CHEMBL52750 | — | — | 1 | 7.28 |
| CHEMBL1269148 | — | — | 1 | 7.23 |
| CHEMBL1270143 | — | — | 1 | 7.23 |
| CHEMBL1269061 | — | — | 1 | 7.22 |
| CHEMBL1270038 | — | — | 1 | 6.96 |
| CHEMBL1269093 | — | — | 1 | 6.91 |
| CHEMBL1269785 | — | — | 1 | 6.91 |
| CHEMBL1269059 | — | — | 1 | 6.91 |
| CHEMBL1270538 | — | — | 1 | 6.86 |
| CHEMBL1270347 | — | — | 1 | 6.84 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1270443 | — | Ki | = | 2.02 | nM | 8.70 |
| CHEMBL1269816 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1270540 | — | Ki | = | 4.54 | nM | 8.34 |
| CHEMBL11709 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL1270638 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1270539 | — | Ki | = | 8.93 | nM | 8.05 |
| CHEMBL1270442 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1270248 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL307783 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1270637 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL299250 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL1269058 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL1270037 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1269786 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1269149 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL1270639 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL1270144 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1269929 | — | Ki | = | 44.6 | nM | 7.35 |
| CHEMBL1269930 | — | Ki | = | 44.9 | nM | 7.35 |
| CHEMBL52750 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL1269148 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1270143 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1269061 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL1270038 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL1269785 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL1269059 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL1269093 | — | Ki | = | 123.6 | nM | 6.91 |
| CHEMBL1270538 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL1270347 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL1270348 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL1270741 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL66902 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL1270247 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL1270943 | — | Ki | = | 343.3 | nM | 6.46 |
| CHEMBL1269094 | — | Ki | = | 818.0 | nM | 6.09 |
| CHEMBL1270843 | — | Ki | = | 931.0 | nM | 6.03 |
| CHEMBL1270841 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1270740 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1269060 | — | Ki | = | 1059.0 | nM | 5.97 |
| CHEMBL13662 | CI-218872 | Ki | = | 1964.0 | nM | 5.71 |
| CHEMBL1270739 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL87331 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL87641 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL1270944 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL1271046 | — | Ki | - | — | - |