Assay Detail
Binding
CHEMBL4005714
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Inhibition of JAK3 in human whole blood assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by IL-15 addition and measured after 15 mins by Alexa Fluor 647 staining based flow cytometric analysis
8
Total Activities
8
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 |
Publication
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.25 | 6.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 6.71 |
| CHEMBL4064018 | — | — | 1 | 6.40 |
| CHEMBL4062946 | — | — | 1 | 6.24 |
| CHEMBL4085582 | — | — | 1 | 5.64 |
| CHEMBL4083094 | — | — | 1 | - |
| CHEMBL4090883 | — | — | 1 | - |
| CHEMBL4075230 | — | — | 1 | - |
| CHEMBL4095629 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4064018 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL4062946 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4085582 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL4083094 | — | IC50 | - | — | - | |
| CHEMBL4090883 | — | IC50 | - | — | - | |
| CHEMBL4075230 | — | IC50 | - | — | - | |
| CHEMBL4095629 | — | IC50 | - | — | - |