Assay Detail
Binding
CHEMBL1249063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat GABA alpha-1-beta-2-gamma-2 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Homology modeling and atomic level binding study of GABA(A) receptor with novel enaminone amides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.04 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426916 | — | — | 1 | 8.15 |
| CHEMBL390326 | — | — | 1 | 7.70 |
| CHEMBL229535 | — | — | 1 | 7.52 |
| CHEMBL387958 | — | — | 1 | 7.52 |
| CHEMBL229534 | — | — | 1 | 7.40 |
| CHEMBL556727 | — | — | 1 | 7.35 |
| CHEMBL229374 | — | — | 1 | 7.30 |
| CHEMBL229201 | — | — | 1 | 7.10 |
| CHEMBL227018 | — | — | 1 | 6.80 |
| CHEMBL388639 | — | — | 1 | 6.40 |
| CHEMBL227017 | — | — | 1 | 5.77 |
| CHEMBL388638 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426916 | — | IC50 | = | 7.079 | nM | 8.15 |
| CHEMBL390326 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL229535 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL387958 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL229534 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL556727 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL229374 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL229201 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL227018 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL388639 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL227017 | — | IC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL388638 | — | IC50 | = | 3019.95 | nM | 5.52 |