Assay Detail
Binding
CHEMBL823141
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1
29
Total Activities
29
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-1 (CHEMBL1962) ↗| 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 | 29 | 6.98 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148740 | — | — | 1 | 7.77 |
| CHEMBL356161 | — | — | 1 | 7.75 |
| CHEMBL356271 | — | — | 1 | 7.55 |
| CHEMBL145910 | — | — | 1 | 7.44 |
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 7.43 |
| CHEMBL147842 | — | — | 1 | 7.39 |
| CHEMBL342270 | — | — | 1 | 7.28 |
| CHEMBL146086 | — | — | 1 | 7.25 |
| CHEMBL356806 | — | — | 1 | 7.16 |
| CHEMBL146356 | — | — | 1 | 7.09 |
| CHEMBL343009 | — | — | 1 | 7.04 |
| CHEMBL146302 | — | — | 1 | 7.03 |
| CHEMBL358519 | — | — | 1 | 7.02 |
| CHEMBL147364 | — | — | 1 | 6.97 |
| CHEMBL358874 | — | — | 1 | 6.93 |
| CHEMBL145983 | — | — | 1 | 6.92 |
| CHEMBL146230 | — | — | 1 | 6.90 |
| CHEMBL147590 | — | — | 1 | 6.88 |
| CHEMBL148044 | — | — | 1 | 6.87 |
| CHEMBL145970 | — | — | 1 | 6.87 |
| CHEMBL358301 | — | — | 1 | 6.77 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.70 |
| CHEMBL148043 | — | — | 1 | 6.68 |
| CHEMBL147379 | — | — | 1 | 6.59 |
| CHEMBL147312 | — | — | 1 | 6.58 |
| CHEMBL343471 | — | — | 1 | 6.52 |
| CHEMBL344120 | — | — | 1 | 6.26 |
| CHEMBL146317 | — | — | 1 | 5.66 |
| CHEMBL146075 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148740 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL356161 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL356271 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL145910 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL661 | ALPRAZOLAM | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL147842 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL342270 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL146086 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL356806 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL146356 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL343009 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL146302 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL358519 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL147364 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL358874 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL145983 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL146230 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL147590 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL148044 | — | EC50 | = | 136.0 | nM | 6.87 |
| CHEMBL145970 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL358301 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL911 | ZOLPIDEM | EC50 | = | 198.0 | nM | 6.70 |
| CHEMBL148043 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL147379 | — | EC50 | = | 258.0 | nM | 6.59 |
| CHEMBL147312 | — | EC50 | = | 266.0 | nM | 6.58 |
| CHEMBL343471 | — | EC50 | = | 303.0 | nM | 6.52 |
| CHEMBL344120 | — | EC50 | = | 544.0 | nM | 6.26 |
| CHEMBL146317 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL146075 | — | EC50 | < | 100.0 | nM | - |