Assay Detail
Binding
CHEMBL678889
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 2
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Xenopus laevis |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gamma-aminobutyric acid receptor subunit alpha-2 (CHEMBL4956) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.74 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 7.92 |
| CHEMBL356161 | — | — | 1 | 7.70 |
| CHEMBL147842 | — | — | 1 | 7.26 |
| CHEMBL147364 | — | — | 1 | 7.17 |
| CHEMBL356806 | — | — | 1 | 7.16 |
| CHEMBL146488 | — | — | 1 | 7.08 |
| CHEMBL342270 | — | — | 1 | 7.00 |
| CHEMBL146086 | — | — | 1 | 7.00 |
| CHEMBL358519 | — | — | 1 | 6.96 |
| CHEMBL344120 | — | — | 1 | 6.87 |
| CHEMBL356271 | — | — | 1 | 6.84 |
| CHEMBL145983 | — | — | 1 | 6.81 |
| CHEMBL148740 | — | — | 1 | 6.74 |
| CHEMBL145910 | — | — | 1 | 6.73 |
| CHEMBL146230 | — | — | 1 | 6.70 |
| CHEMBL343009 | — | — | 1 | 6.68 |
| CHEMBL147590 | — | — | 1 | 6.62 |
| CHEMBL147379 | — | — | 1 | 6.61 |
| CHEMBL148044 | — | — | 1 | 6.61 |
| CHEMBL146302 | — | — | 1 | 6.59 |
| CHEMBL146356 | — | — | 1 | 6.57 |
| CHEMBL358301 | — | — | 1 | 6.55 |
| CHEMBL343471 | — | — | 1 | 6.49 |
| CHEMBL146317 | — | — | 1 | 6.42 |
| CHEMBL358874 | — | — | 1 | 6.34 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.13 |
| CHEMBL148043 | — | — | 1 | 6.06 |
| CHEMBL145970 | — | — | 1 | 5.93 |
| CHEMBL147312 | — | — | 1 | 5.93 |
| CHEMBL146075 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL661 | ALPRAZOLAM | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL356161 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL147842 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL147364 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL356806 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL146488 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL342270 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL146086 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL358519 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL344120 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL356271 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL145983 | — | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL148740 | — | EC50 | = | 184.0 | nM | 6.74 |
| CHEMBL145910 | — | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL146230 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL343009 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL147590 | — | EC50 | = | 238.0 | nM | 6.62 |
| CHEMBL147379 | — | EC50 | = | 247.0 | nM | 6.61 |
| CHEMBL148044 | — | EC50 | = | 245.0 | nM | 6.61 |
| CHEMBL146302 | — | EC50 | = | 256.0 | nM | 6.59 |
| CHEMBL146356 | — | EC50 | = | 268.0 | nM | 6.57 |
| CHEMBL358301 | — | EC50 | = | 284.0 | nM | 6.55 |
| CHEMBL343471 | — | EC50 | = | 327.0 | nM | 6.49 |
| CHEMBL146317 | — | EC50 | = | 383.0 | nM | 6.42 |
| CHEMBL358874 | — | EC50 | = | 459.0 | nM | 6.34 |
| CHEMBL911 | ZOLPIDEM | EC50 | = | 737.0 | nM | 6.13 |
| CHEMBL148043 | — | EC50 | = | 879.0 | nM | 6.06 |
| CHEMBL145970 | — | EC50 | = | 1162.0 | nM | 5.93 |
| CHEMBL147312 | — | EC50 | = | 1179.0 | nM | 5.93 |
| CHEMBL146075 | — | EC50 | < | 100.0 | nM | - |