Assay Detail
Binding
CHEMBL831818
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against GABA-evoked chloride currents mediated by human Gamma-aminobutyric acid GABA-A receptor alpha2-beta2-gamma2L expressed in Xenopus oocytes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Target
GABA A receptor alpha-2/beta-2/gamma-2 (CHEMBL2111413) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 5.54 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426988 | — | — | 1 | 6.72 |
| CHEMBL365317 | — | — | 1 | 6.35 |
| CHEMBL193243 | — | — | 1 | 6.22 |
| CHEMBL192969 | — | — | 1 | 6.00 |
| CHEMBL192127 | — | — | 1 | 5.89 |
| CHEMBL192900 | — | — | 1 | 5.82 |
| CHEMBL190255 | — | — | 1 | 5.77 |
| CHEMBL189594 | — | — | 1 | 5.75 |
| CHEMBL364296 | — | — | 1 | 5.72 |
| CHEMBL190279 | ALFAXALONE | 2.0 | 1 | 5.70 |
| CHEMBL444016 | — | — | 1 | 5.64 |
| CHEMBL192819 | — | — | 1 | 5.62 |
| CHEMBL193092 | — | — | 1 | 5.52 |
| CHEMBL426986 | — | — | 1 | 5.51 |
| CHEMBL190131 | — | — | 1 | 5.47 |
| CHEMBL681 | ETOMIDATE | 4.0 | 1 | 5.46 |
| CHEMBL189596 | — | — | 1 | 5.39 |
| CHEMBL193201 | — | — | 1 | 5.38 |
| CHEMBL190358 | — | — | 1 | 5.37 |
| CHEMBL190596 | — | — | 1 | 5.36 |
| CHEMBL190737 | — | — | 1 | 5.19 |
| CHEMBL192498 | — | — | 1 | 5.06 |
| CHEMBL192524 | — | — | 1 | 5.04 |
| CHEMBL526 | PROPOFOL | 4.0 | 1 | 4.95 |
| CHEMBL425732 | — | — | 1 | 4.72 |
| CHEMBL448 | PENTOBARBITAL | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426988 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL365317 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL193243 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL192969 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL192127 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL192900 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL190255 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL189594 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL364296 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL190279 | ALFAXALONE | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL444016 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL192819 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL193092 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL426986 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL190131 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL681 | ETOMIDATE | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL189596 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL193201 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL190358 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL190596 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL190737 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL192498 | — | EC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL192524 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL526 | PROPOFOL | EC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL425732 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL448 | PENTOBARBITAL | EC50 | = | 50000.0 | nM | 4.30 |