Assay Detail
Binding
CHEMBL4340978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG incubated for 1 hr by Fluorescence polarization binding assay
13
Total Activities
13
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 novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.50 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 6.29 |
| CHEMBL4483071 | — | — | 1 | 5.68 |
| CHEMBL1952142 | — | — | 1 | 5.68 |
| CHEMBL4521827 | — | — | 1 | 5.40 |
| CHEMBL4449598 | — | — | 1 | 5.22 |
| CHEMBL4576509 | — | — | 1 | 4.71 |
| CHEMBL4468395 | — | — | 1 | - |
| CHEMBL4543342 | — | — | 1 | - |
| CHEMBL4547383 | — | — | 1 | - |
| CHEMBL4556293 | — | — | 1 | - |
| CHEMBL4526558 | — | — | 1 | - |
| CHEMBL4527736 | — | — | 1 | - |
| CHEMBL4460019 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1952329 | SGI-1776 | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL4483071 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1952142 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4521827 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4449598 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL4576509 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL4468395 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4543342 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4547383 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4556293 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4526558 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4527736 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4460019 | — | IC50 | > | 20000.0 | nM | - |