Assay Detail
Binding
CHEMBL4398029
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Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transiently expressed in human tsA201 cells incubated for 30 mins and measured up to 90 secs by FMP dye based FLIPR membrane potential blue assay
34
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 5.04 | 5.82 |
| pEC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4547372 | — | — | 2 | 5.82 |
| CHEMBL79325 | — | — | 2 | 5.75 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 5.43 |
| CHEMBL4458674 | — | — | 2 | 5.12 |
| CHEMBL4442696 | — | — | 2 | 5.01 |
| CHEMBL4526098 | — | — | 2 | 4.96 |
| CHEMBL4554798 | — | — | 2 | 4.92 |
| CHEMBL1788265 | — | — | 2 | 4.92 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 2 | 4.62 |
| CHEMBL4464494 | — | — | 4 | 4.60 |
| CHEMBL4455221 | — | — | 2 | 4.32 |
| CHEMBL4566832 | — | — | 2 | - |
| CHEMBL4586460 | — | — | 2 | - |
| CHEMBL4471977 | — | — | 2 | - |
| CHEMBL349005 | — | — | 2 | - |
| CHEMBL71460 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4547372 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4547372 | — | EC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL79325 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL79325 | — | EC50 | = | 1862.09 | nM | 5.73 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL4458674 | — | EC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL4458674 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4442696 | — | EC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4442696 | — | EC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL4526098 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4526098 | — | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL1788265 | — | EC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL1788265 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4554798 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4554798 | — | EC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | EC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL4464494 | — | EC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4464494 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4455221 | — | EC50 | = | 47863.01 | nM | 4.32 |
| CHEMBL4455221 | — | EC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL71460 | — | EC50 | - | — | - | |
| CHEMBL349005 | — | EC50 | - | — | - | |
| CHEMBL4471977 | — | EC50 | - | — | - | |
| CHEMBL4586460 | — | EC50 | - | — | - | |
| CHEMBL4566832 | — | EC50 | - | — | - | |
| CHEMBL4464494 | — | EC50 | - | — | - | |
| CHEMBL71460 | — | pEC50 | - | — | - | |
| CHEMBL349005 | — | pEC50 | - | — | - | |
| CHEMBL4471977 | — | pEC50 | - | — | - | |
| CHEMBL4586460 | — | pEC50 | - | — | - | |
| CHEMBL4566832 | — | pEC50 | - | — | - | |
| CHEMBL4464494 | — | pEC50 | - | — | - |