Assay Detail
Binding
CHEMBL4482009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human JAK2 using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and further incubated for 30 mins and subsequently measured after 1 hr by HTRF assay
31
Total Activities
31
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
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.31 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.30 |
| CHEMBL4589415 | — | — | 1 | 6.55 |
| CHEMBL4581532 | — | — | 1 | 6.46 |
| CHEMBL4516549 | — | — | 1 | 6.46 |
| CHEMBL4591192 | — | — | 1 | 6.44 |
| CHEMBL4524497 | — | — | 1 | 6.30 |
| CHEMBL4566849 | — | — | 1 | 6.04 |
| CHEMBL3601722 | — | — | 1 | 6.03 |
| CHEMBL4546009 | — | — | 1 | 5.99 |
| CHEMBL4573218 | — | — | 1 | 5.96 |
| CHEMBL4518786 | — | — | 1 | 5.84 |
| CHEMBL4574614 | — | — | 1 | 5.69 |
| CHEMBL4541547 | — | — | 1 | 5.68 |
| CHEMBL4525246 | — | — | 1 | 5.55 |
| CHEMBL4539137 | — | — | 1 | - |
| CHEMBL4526018 | — | — | 1 | - |
| CHEMBL4572373 | — | — | 1 | - |
| CHEMBL4593058 | — | — | 1 | - |
| CHEMBL4577029 | — | — | 1 | - |
| CHEMBL4566777 | — | — | 1 | - |
| CHEMBL4537782 | — | — | 1 | - |
| CHEMBL4588496 | — | — | 1 | - |
| CHEMBL4521305 | — | — | 1 | - |
| CHEMBL4555932 | — | — | 1 | - |
| CHEMBL4587735 | — | — | 1 | - |
| CHEMBL4560222 | — | — | 1 | - |
| CHEMBL4528217 | — | — | 1 | - |
| CHEMBL4552985 | — | — | 1 | - |
| CHEMBL4563864 | — | — | 1 | - |
| CHEMBL4571470 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4589415 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4581532 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4516549 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL4591192 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL4524497 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL4566849 | — | IC50 | = | 916.0 | nM | 6.04 |
| CHEMBL3601722 | — | IC50 | = | 945.0 | nM | 6.03 |
| CHEMBL4546009 | — | IC50 | = | 1015.0 | nM | 5.99 |
| CHEMBL4573218 | — | IC50 | = | 1096.0 | nM | 5.96 |
| CHEMBL4518786 | — | IC50 | = | 1444.0 | nM | 5.84 |
| CHEMBL4574614 | — | IC50 | = | 2043.0 | nM | 5.69 |
| CHEMBL4541547 | — | IC50 | = | 2098.0 | nM | 5.68 |
| CHEMBL4525246 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL4556768 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4539137 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4526018 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4572373 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4593058 | — | IC50 | - | — | - | |
| CHEMBL4577029 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4566777 | — | IC50 | - | — | - | |
| CHEMBL4537782 | — | IC50 | - | — | - | |
| CHEMBL4588496 | — | IC50 | - | — | - | |
| CHEMBL4521305 | — | IC50 | - | — | - | |
| CHEMBL4555932 | — | IC50 | - | — | - | |
| CHEMBL4587735 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4560222 | — | IC50 | - | — | - | |
| CHEMBL4528217 | — | IC50 | - | — | - | |
| CHEMBL4552985 | — | IC50 | - | — | - | |
| CHEMBL4563864 | — | IC50 | - | — | - | |
| CHEMBL4571470 | — | IC50 | - | — | - |