Assay Detail
Binding
CHEMBL4201937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by patch clamp method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.89 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204675 | — | — | 1 | 5.58 |
| CHEMBL4216339 | — | — | 1 | 5.11 |
| CHEMBL4216862 | — | — | 1 | 5.02 |
| CHEMBL4211893 | — | — | 1 | 4.87 |
| CHEMBL4209441 | SOFNOBRUTINIB | 2.0 | 1 | 4.62 |
| CHEMBL4208062 | — | — | 1 | 4.52 |
| CHEMBL4203192 | — | — | 1 | 4.52 |
| CHEMBL4217816 | — | — | 1 | - |
| CHEMBL4214343 | — | — | 1 | - |
| CHEMBL4212436 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204675 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4216339 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4216862 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4211893 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL4209441 | SOFNOBRUTINIB | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4208062 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4203192 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4217816 | — | IC50 | - | — | - | |
| CHEMBL4214343 | — | IC50 | - | — | - | |
| CHEMBL4212436 | — | IC50 | - | — | - |