Assay Detail
Binding
CHEMBL2423449
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins by FLIPR membrane potential blue assay
17
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | tsA201 |
| 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
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.85 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2420450 | — | — | 2 | 6.68 |
| CHEMBL1091277 | — | — | 1 | 6.68 |
| CHEMBL32503 | GABAZINE | — | 1 | 6.62 |
| CHEMBL2420454 | — | — | 2 | 6.16 |
| CHEMBL2420455 | — | — | 2 | 6.11 |
| CHEMBL2420449 | — | — | 2 | 5.01 |
| CHEMBL2420447 | — | — | 2 | 4.52 |
| CHEMBL2420453 | — | — | 1 | - |
| CHEMBL2420452 | — | — | 1 | - |
| CHEMBL2420451 | — | — | 1 | - |
| CHEMBL2420448 | — | — | 1 | - |
| CHEMBL1090917 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2420450 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1091277 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2420450 | — | IC50 | = | 213.8 | nM | 6.67 |
| CHEMBL32503 | GABAZINE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2420454 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL2420454 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL2420455 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2420455 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL2420449 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL2420449 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL2420447 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2420447 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL2420452 | — | IC50 | - | — | - | |
| CHEMBL2420451 | — | IC50 | - | — | - | |
| CHEMBL2420448 | — | IC50 | - | — | - | |
| CHEMBL1090917 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL2420453 | — | IC50 | - | — | - |