Assay Detail
Binding
CHEMBL4033008
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]-MK499 from human ERG expressed in HEK293 cell membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.55 | 4.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3703085 | — | — | 1 | 4.91 |
| CHEMBL4096821 | — | — | 1 | 4.88 |
| CHEMBL4102140 | — | — | 1 | 4.60 |
| CHEMBL3647849 | — | — | 1 | 4.58 |
| CHEMBL3703025 | — | — | 1 | 4.50 |
| CHEMBL4077886 | — | — | 1 | 4.46 |
| CHEMBL4089234 | — | — | 1 | 4.40 |
| CHEMBL4104623 | — | — | 1 | 4.40 |
| CHEMBL4061128 | — | — | 1 | 4.40 |
| CHEMBL4094682 | — | — | 1 | 4.34 |
| CHEMBL4076821 | — | — | 1 | - |
| CHEMBL4100288 | — | — | 1 | - |
| CHEMBL4078799 | — | — | 1 | - |
| CHEMBL4067915 | — | — | 1 | - |
| CHEMBL4089118 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3703085 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4096821 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL4102140 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3647849 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3703025 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4077886 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4089234 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4104623 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4061128 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4094682 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL4076821 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4100288 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4078799 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4067915 | — | IC50 | > | 60000.0 | nM | - |
| CHEMBL4089118 | — | IC50 | > | 60000.0 | nM | - |