Assay Detail
Binding
CHEMBL4675676
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Inhibition of human ERG by plate-based planar patch clamp method
16
Total Activities
16
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
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.16 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784088 | — | — | 1 | 5.66 |
| CHEMBL4751083 | — | — | 1 | 5.52 |
| CHEMBL4753141 | — | — | 1 | 5.44 |
| CHEMBL4786316 | — | — | 1 | 5.35 |
| CHEMBL4762290 | — | — | 1 | 5.31 |
| CHEMBL4753469 | — | — | 1 | 5.14 |
| CHEMBL4792651 | — | — | 1 | 5.00 |
| CHEMBL4752008 | — | — | 1 | 4.96 |
| CHEMBL4780257 | — | — | 1 | 4.92 |
| CHEMBL4784783 | — | — | 1 | 4.85 |
| CHEMBL4744190 | — | — | 1 | 4.64 |
| CHEMBL3622956 | — | — | 1 | - |
| CHEMBL4793844 | — | — | 1 | - |
| CHEMBL4757235 | — | — | 1 | - |
| CHEMBL4790107 | — | — | 1 | - |
| CHEMBL4753164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784088 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4751083 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4753141 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4786316 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4762290 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4753469 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4792651 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4752008 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4780257 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4784783 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4744190 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3622956 | — | IC50 | - | — | - | |
| CHEMBL4793844 | — | IC50 | - | — | - | |
| CHEMBL4757235 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4790107 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4753164 | — | IC50 | > | 40000.0 | nM | - |