Assay Detail
Binding
CHEMBL4005715
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged cytoplasmic JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of 4 uM ATP by microfluidic assay
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 | 8.09 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085582 | — | — | 1 | 9.52 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 9.52 |
| CHEMBL4064018 | — | — | 1 | 9.40 |
| CHEMBL4062946 | — | — | 1 | 9.15 |
| CHEMBL4090883 | — | — | 1 | 7.75 |
| CHEMBL4083094 | — | — | 1 | 7.12 |
| CHEMBL4075230 | — | — | 1 | 6.43 |
| CHEMBL4095629 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085582 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4064018 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4062946 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4090883 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4083094 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4075230 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4095629 | — | IC50 | = | 1610.0 | nM | 5.79 |