Assay Detail
Functional
CHEMBL1799216
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.70 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795561 | — | — | 1 | 8.52 |
| CHEMBL1795560 | — | — | 1 | 8.15 |
| CHEMBL1795348 | — | — | 1 | 7.96 |
| CHEMBL1795562 | — | — | 1 | 7.40 |
| CHEMBL32503 | GABAZINE | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795561 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1795560 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1795348 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1795562 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL32503 | GABAZINE | IC50 | = | 349.0 | nM | 6.46 |