Assay Detail
Binding
CHEMBL1772131
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Inhibition of human ASIC3 expressed in HEK293 cells assessed as inhibition of acid-evoked current by manual patch-clamp electrophysiology assay
25
Total Activities
25
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
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 4.65 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770740 | — | — | 1 | 5.92 |
| CHEMBL1770745 | — | — | 1 | 5.77 |
| CHEMBL1770739 | — | — | 1 | 5.58 |
| CHEMBL1770750 | — | — | 1 | 5.51 |
| CHEMBL1770744 | — | — | 1 | 5.48 |
| CHEMBL1770752 | — | — | 1 | 5.42 |
| CHEMBL1770741 | — | — | 1 | 5.24 |
| CHEMBL1770738 | — | — | 1 | 5.16 |
| CHEMBL1770746 | — | — | 1 | 5.15 |
| CHEMBL1770730 | — | — | 1 | 5.05 |
| CHEMBL1770753 | — | — | 1 | 5.02 |
| CHEMBL1770743 | — | — | 1 | 4.96 |
| CHEMBL1770749 | — | — | 1 | 4.84 |
| CHEMBL1770751 | — | — | 1 | 4.77 |
| CHEMBL1770748 | — | — | 1 | 4.71 |
| CHEMBL1770742 | — | — | 1 | 4.56 |
| CHEMBL1770735 | — | — | 1 | 4.01 |
| CHEMBL1770733 | — | — | 1 | 3.89 |
| CHEMBL1770737 | — | — | 1 | 3.80 |
| CHEMBL196536 | — | — | 1 | 3.72 |
| CHEMBL1770734 | — | — | 1 | 3.44 |
| CHEMBL1770736 | — | — | 1 | 3.37 |
| CHEMBL1770731 | — | — | 1 | 3.15 |
| CHEMBL1671950 | — | — | 1 | 3.12 |
| CHEMBL1770747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770740 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1770745 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1770739 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1770750 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1770744 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1770752 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1770741 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1770738 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1770746 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL1770730 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1770753 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL1770743 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL1770749 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL1770751 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1770748 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL1770742 | — | IC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL1770735 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL1770733 | — | IC50 | = | 130000.0 | nM | 3.89 |
| CHEMBL1770737 | — | IC50 | = | 160000.0 | nM | 3.80 |
| CHEMBL196536 | — | IC50 | = | 190000.0 | nM | 3.72 |
| CHEMBL1770734 | — | IC50 | = | 363000.0 | nM | 3.44 |
| CHEMBL1770736 | — | IC50 | = | 430000.0 | nM | 3.37 |
| CHEMBL1770731 | — | IC50 | = | 701000.0 | nM | 3.15 |
| CHEMBL1671950 | — | IC50 | = | 763000.0 | nM | 3.12 |
| CHEMBL1770747 | — | IC50 | = | 103000.0 | nM | - |