Assay Detail
Binding
CHEMBL2396019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK cells by ion flux electrophysiology method
9
Total Activities
9
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 |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.93 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2391939 | — | — | 1 | 7.42 |
| CHEMBL2391795 | — | — | 1 | 6.52 |
| CHEMBL2391800 | — | — | 1 | 6.16 |
| CHEMBL2391935 | — | — | 1 | 5.92 |
| CHEMBL2391810 | — | — | 1 | 5.80 |
| CHEMBL2391803 | — | — | 1 | 5.08 |
| CHEMBL2391804 | — | — | 1 | 4.64 |
| CHEMBL2391797 | — | — | 1 | - |
| CHEMBL2391807 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2391939 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2391795 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2391800 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2391935 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2391810 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2391803 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL2391804 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL2391797 | — | IC50 | > | 17500.0 | nM | - |
| CHEMBL2391807 | — | IC50 | > | 10000.0 | nM | - |