Assay Detail
Binding
CHEMBL1838283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO-K1 cells after 2 hrs by Cy3b-Dofetilide-based fluorescence polarisation assay
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.51 | 6.30 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1835057 | — | — | 1 | 6.30 |
| CHEMBL1835063 | — | — | 1 | 6.10 |
| CHEMBL1835061 | — | — | 1 | 6.00 |
| CHEMBL1834758 | — | — | 1 | 5.80 |
| CHEMBL1835059 | — | — | 1 | 5.80 |
| CHEMBL515757 | — | — | 1 | 5.70 |
| CHEMBL1835058 | — | — | 1 | 5.60 |
| CHEMBL1835060 | — | — | 1 | 5.60 |
| CHEMBL1834757 | — | — | 1 | 5.60 |
| CHEMBL1835062 | — | — | 1 | 5.60 |
| CHEMBL1235110 | — | — | 1 | 5.50 |
| CHEMBL1835068 | — | — | 1 | 5.50 |
| CHEMBL1835065 | — | — | 1 | 5.40 |
| CHEMBL1835067 | — | — | 1 | 5.40 |
| CHEMBL1835064 | — | — | 1 | 5.20 |
| CHEMBL1835066 | — | — | 1 | 5.10 |
| CHEMBL1835069 | — | — | 1 | 5.10 |
| CHEMBL1835071 | — | — | 1 | 4.70 |
| CHEMBL1835070 | — | — | 1 | 4.60 |
| CHEMBL1835072 | — | — | 1 | - |
| CHEMBL1834756 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1835057 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL1835063 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL1835061 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1834758 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL1835059 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL515757 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL1835058 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1835060 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1834757 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1835062 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1235110 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1835068 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1835065 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL1835067 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL1835064 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL1835066 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL1835069 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL1835071 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL1835070 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL1835072 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL1834756 | — | pIC50 | - | — | - |