Assay Detail
Binding
CHEMBL4685309
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged JAK3 cytoplasmic domain (781 to 1124 residues) expressed in baculovirus expression system using TK-substrate-biotin preincubated for 5 mins followed by substrate addition and measured after 30 mins by HTRF assay
40
Total Activities
40
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, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.16 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.05 |
| CHEMBL4746272 | — | — | 1 | 8.77 |
| CHEMBL4750184 | — | — | 1 | 8.21 |
| CHEMBL4780984 | — | — | 1 | 8.04 |
| CHEMBL4782611 | — | — | 1 | 7.85 |
| CHEMBL1078166 | — | — | 1 | 7.82 |
| CHEMBL4744519 | — | — | 1 | 7.62 |
| CHEMBL4763424 | — | — | 1 | 7.54 |
| CHEMBL4758891 | — | — | 1 | 7.52 |
| CHEMBL4743357 | — | — | 1 | 7.48 |
| CHEMBL4778980 | — | — | 1 | 7.46 |
| CHEMBL4754557 | — | — | 1 | 7.26 |
| CHEMBL4741588 | — | — | 1 | 7.19 |
| CHEMBL4756648 | — | — | 1 | 7.18 |
| CHEMBL4750671 | — | — | 1 | 7.17 |
| CHEMBL4756089 | — | — | 1 | 7.17 |
| CHEMBL4777465 | — | — | 1 | 7.12 |
| CHEMBL4740169 | — | — | 1 | 7.11 |
| CHEMBL4755671 | — | — | 1 | 7.07 |
| CHEMBL4754061 | — | — | 1 | 7.04 |
| CHEMBL4762354 | — | — | 1 | 7.02 |
| CHEMBL4793519 | — | — | 1 | 7.00 |
| CHEMBL4747498 | — | — | 1 | 7.00 |
| CHEMBL4796206 | — | — | 1 | 6.99 |
| CHEMBL4758931 | — | — | 1 | 6.97 |
| CHEMBL4749364 | — | — | 1 | 6.95 |
| CHEMBL4746760 | — | — | 1 | 6.90 |
| CHEMBL4777645 | — | — | 1 | 6.86 |
| CHEMBL4753620 | — | — | 1 | 6.84 |
| CHEMBL1077575 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4746272 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4750184 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4780984 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4782611 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1078166 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4744519 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4763424 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4758891 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4743357 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4778980 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4754557 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4741588 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4756648 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4756089 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4750671 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4777465 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4740169 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4755671 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4754061 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4762354 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4747498 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4793519 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4796206 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4758931 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4749364 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4746760 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4777645 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4753620 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL1077575 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4778274 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4761545 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4740191 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4739907 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4780644 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL4789894 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL4750831 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL4795109 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL4740889 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL4778584 | — | IC50 | = | 599.0 | nM | 6.22 |