Assay Detail
Binding
CHEMBL4723228
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG channel in presence of dofetilide by competition binding assay
21
Total Activities
21
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 Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.96 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764678 | — | — | 1 | 6.30 |
| CHEMBL4791610 | — | — | 1 | 5.17 |
| CHEMBL4752511 | — | — | 1 | 5.07 |
| CHEMBL4785725 | — | — | 1 | 5.00 |
| CHEMBL4780066 | — | — | 1 | 4.96 |
| CHEMBL4779862 | — | — | 1 | 4.92 |
| CHEMBL4752290 | — | — | 1 | 4.89 |
| CHEMBL4745615 | — | — | 1 | 4.75 |
| CHEMBL4777580 | — | — | 1 | 4.70 |
| CHEMBL4778828 | — | — | 1 | 4.66 |
| CHEMBL3955498 | — | — | 1 | 4.60 |
| CHEMBL4744460 | — | — | 1 | 4.55 |
| CHEMBL3905155 | — | — | 1 | - |
| CHEMBL4790514 | — | — | 1 | - |
| CHEMBL4786195 | — | — | 1 | - |
| CHEMBL4754106 | — | — | 1 | - |
| CHEMBL3973674 | — | — | 1 | - |
| CHEMBL4781381 | — | — | 1 | - |
| CHEMBL4789692 | — | — | 1 | - |
| CHEMBL4787060 | — | — | 1 | - |
| CHEMBL4758510 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764678 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4791610 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4752511 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4785725 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4780066 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4779862 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4752290 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4745615 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4777580 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4778828 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3955498 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4744460 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3905155 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4790514 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4786195 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4754106 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3973674 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4781381 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4789692 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4787060 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4758510 | — | IC50 | > | 30000.0 | nM | - |