Assay Detail
Binding
CHEMBL1954570
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG expressed in CHO-K1 cell membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.38 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1952144 | — | — | 1 | 6.40 |
| CHEMBL1952141 | — | — | 1 | 5.50 |
| CHEMBL1952142 | — | — | 1 | 5.50 |
| CHEMBL1952113 | — | — | 1 | 5.00 |
| CHEMBL1952143 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1952144 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL1952141 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1952142 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1952113 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1952143 | — | IC50 | = | 31622.78 | nM | 4.50 |