Assay Detail
ADMET
CHEMBL4685311
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged JAK1 cytoplasmic domain (866 to 1154 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 | ADMET |
| 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 | 6.17 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.89 |
| CHEMBL4758931 | — | — | 1 | 7.35 |
| CHEMBL4756648 | — | — | 1 | 7.25 |
| CHEMBL4762354 | — | — | 1 | 7.05 |
| CHEMBL4744519 | — | — | 1 | 6.74 |
| CHEMBL4747498 | — | — | 1 | 6.49 |
| CHEMBL4741588 | — | — | 1 | 6.49 |
| CHEMBL4796206 | — | — | 1 | 6.45 |
| CHEMBL1078166 | — | — | 1 | 6.36 |
| CHEMBL4740169 | — | — | 1 | 6.28 |
| CHEMBL4793519 | — | — | 1 | 6.25 |
| CHEMBL4795109 | — | — | 1 | 6.23 |
| CHEMBL4789894 | — | — | 1 | 6.18 |
| CHEMBL4750831 | — | — | 1 | 6.14 |
| CHEMBL4777645 | — | — | 1 | 6.08 |
| CHEMBL4753620 | — | — | 1 | 6.07 |
| CHEMBL4750671 | — | — | 1 | 6.05 |
| CHEMBL4749364 | — | — | 1 | 6.02 |
| CHEMBL4754557 | — | — | 1 | 5.96 |
| CHEMBL4761545 | — | — | 1 | 5.96 |
| CHEMBL4750184 | — | — | 1 | 5.94 |
| CHEMBL4763424 | — | — | 1 | 5.89 |
| CHEMBL4746272 | — | — | 1 | 5.88 |
| CHEMBL4780644 | — | — | 1 | 5.84 |
| CHEMBL4782611 | — | — | 1 | 5.84 |
| CHEMBL4740889 | — | — | 1 | 5.82 |
| CHEMBL4780984 | — | — | 1 | 5.81 |
| CHEMBL4739907 | — | — | 1 | 5.81 |
| CHEMBL4756089 | — | — | 1 | 5.78 |
| CHEMBL4778274 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4758931 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4756648 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4762354 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4744519 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4747498 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4741588 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL4796206 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL1078166 | — | IC50 | = | 433.0 | nM | 6.36 |
| CHEMBL4740169 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL4793519 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL4795109 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL4789894 | — | IC50 | = | 657.0 | nM | 6.18 |
| CHEMBL4750831 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL4777645 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4753620 | — | IC50 | = | 854.0 | nM | 6.07 |
| CHEMBL4750671 | — | IC50 | = | 899.0 | nM | 6.05 |
| CHEMBL4749364 | — | IC50 | = | 961.0 | nM | 6.02 |
| CHEMBL4754557 | — | IC50 | = | 1102.0 | nM | 5.96 |
| CHEMBL4761545 | — | IC50 | = | 1107.0 | nM | 5.96 |
| CHEMBL4750184 | — | IC50 | = | 1147.0 | nM | 5.94 |
| CHEMBL4763424 | — | IC50 | = | 1286.0 | nM | 5.89 |
| CHEMBL4746272 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4780644 | — | IC50 | = | 1432.0 | nM | 5.84 |
| CHEMBL4782611 | — | IC50 | = | 1445.0 | nM | 5.84 |
| CHEMBL4740889 | — | IC50 | = | 1521.0 | nM | 5.82 |
| CHEMBL4780984 | — | IC50 | = | 1562.0 | nM | 5.81 |
| CHEMBL4739907 | — | IC50 | = | 1542.0 | nM | 5.81 |
| CHEMBL4756089 | — | IC50 | = | 1658.0 | nM | 5.78 |
| CHEMBL4778274 | — | IC50 | = | 1861.0 | nM | 5.73 |
| CHEMBL4758891 | — | IC50 | = | 2119.0 | nM | 5.67 |
| CHEMBL1077575 | — | IC50 | = | 2233.0 | nM | 5.65 |
| CHEMBL4740191 | — | IC50 | = | 2443.0 | nM | 5.61 |
| CHEMBL4755671 | — | IC50 | = | 2677.0 | nM | 5.57 |
| CHEMBL4777465 | — | IC50 | = | 2764.0 | nM | 5.56 |
| CHEMBL4778980 | — | IC50 | = | 2876.0 | nM | 5.54 |
| CHEMBL4743357 | — | IC50 | - | — | - | |
| CHEMBL4746760 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4778584 | — | IC50 | - | — | - | |
| CHEMBL4754061 | — | IC50 | - | — | - |