Assay Detail
Binding
CHEMBL4375199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by HPLC analysis
5
Total Activities
5
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
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 5.91 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554990 | — | — | 1 | 6.28 |
| CHEMBL4515024 | — | — | 1 | 6.11 |
| CHEMBL4441219 | — | — | 1 | 5.89 |
| CHEMBL4469908 | — | — | 1 | 5.75 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554990 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL4515024 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL4441219 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4469908 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4072833 | EVOBRUTINIB | Ki | = | 3100.0 | nM | 5.51 |