Assay Detail
Binding
CHEMBL4057949
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by [35S]-MK499 displacement or iKr channel assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.41 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077588 | — | — | 1 | 7.00 |
| CHEMBL4086348 | — | — | 1 | 6.40 |
| CHEMBL4079225 | — | — | 1 | 5.75 |
| CHEMBL4079820 | — | — | 1 | 5.62 |
| CHEMBL4104254 | — | — | 1 | 5.60 |
| CHEMBL4069387 | — | — | 1 | 5.55 |
| CHEMBL4094125 | — | — | 1 | 5.46 |
| CHEMBL4076024 | — | — | 1 | 5.35 |
| CHEMBL4060757 | — | — | 1 | 5.34 |
| CHEMBL4097247 | — | — | 1 | 5.24 |
| CHEMBL4059723 | — | — | 1 | 4.85 |
| CHEMBL4075605 | — | — | 1 | 4.84 |
| CHEMBL4075954 | — | — | 1 | 4.82 |
| CHEMBL4065907 | — | — | 1 | 4.72 |
| CHEMBL4062498 | — | — | 1 | 4.62 |
| CHEMBL4081661 | — | — | 1 | - |
| CHEMBL4087095 | — | — | 1 | - |
| CHEMBL4104951 | — | — | 1 | - |
| CHEMBL4099975 | — | — | 1 | - |
| CHEMBL4096526 | — | — | 1 | - |
| CHEMBL4078497 | — | — | 1 | - |
| CHEMBL4066585 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077588 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4086348 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4079225 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4079820 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4104254 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4069387 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4094125 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4076024 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4060757 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4097247 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4059723 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4075605 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL4075954 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4065907 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4062498 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4081661 | — | IC50 | - | — | - | |
| CHEMBL4087095 | — | IC50 | - | — | - | |
| CHEMBL4104951 | — | IC50 | - | — | - | |
| CHEMBL4099975 | — | IC50 | - | — | - | |
| CHEMBL4096526 | — | IC50 | - | — | - | |
| CHEMBL4078497 | — | IC50 | - | — | - | |
| CHEMBL4066585 | — | IC50 | - | — | - |