Assay Detail
Binding
CHEMBL5227706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ASIC1a in HEK293 cells assessed as inward proton-gated current at pH 6.0 incubated with compound followed by PcTx1 addition by patch-clamp electrophysiology
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Characterization of Novel Mono- and Bis-Guanyl Hydrazones as Potent and Selective ASIC1 Inhibitors Able to Reduce Brain Ischemic Insult.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.79 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5269133 | — | — | 1 | 6.39 |
| CHEMBL5270983 | — | — | 1 | 6.29 |
| CHEMBL5289168 | — | — | 1 | 6.14 |
| CHEMBL5278611 | — | — | 1 | 6.01 |
| CHEMBL5287933 | — | — | 1 | 5.85 |
| CHEMBL5285672 | — | — | 1 | 5.70 |
| CHEMBL5291421 | — | — | 1 | 5.70 |
| CHEMBL5267130 | — | — | 1 | 5.59 |
| CHEMBL5276647 | — | — | 1 | 5.53 |
| CHEMBL5267106 | — | — | 1 | 5.50 |
| CHEMBL5283083 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5269133 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL5270983 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL5289168 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL5278611 | — | IC50 | = | 972.0 | nM | 6.01 |
| CHEMBL5287933 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL5285672 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL5291421 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL5267130 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL5276647 | — | IC50 | = | 2948.0 | nM | 5.53 |
| CHEMBL5267106 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL5283083 | — | IC50 | = | 9538.0 | nM | 5.02 |