Assay Detail
Binding
CHEMBL4265554
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Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of 1 mM ATP concentration by coupled PK/LDH assay
30
Total Activities
30
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
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.70 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4277610 | — | — | 1 | 7.96 |
| CHEMBL4285555 | — | — | 1 | 7.85 |
| CHEMBL4277193 | — | — | 1 | 7.80 |
| CHEMBL4288086 | — | — | 1 | 7.51 |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 7.48 |
| CHEMBL4281035 | — | — | 1 | 7.42 |
| CHEMBL4292320 | — | — | 1 | 7.42 |
| CHEMBL4280180 | — | — | 1 | 7.31 |
| CHEMBL4287845 | — | — | 1 | 7.31 |
| CHEMBL4279720 | — | — | 1 | 7.25 |
| CHEMBL4292341 | — | — | 1 | 7.11 |
| CHEMBL4293778 | — | — | 1 | 7.04 |
| CHEMBL4288935 | — | — | 1 | 6.96 |
| CHEMBL4294868 | — | — | 1 | 6.79 |
| CHEMBL4281393 | — | — | 1 | 6.59 |
| CHEMBL4281693 | — | — | 1 | 6.55 |
| CHEMBL4284396 | — | — | 1 | 6.34 |
| CHEMBL4278647 | — | — | 1 | 6.22 |
| CHEMBL4292010 | — | — | 1 | 6.15 |
| CHEMBL4284952 | — | — | 1 | 6.11 |
| CHEMBL4288201 | — | — | 1 | 5.92 |
| CHEMBL4292612 | — | — | 1 | 5.91 |
| CHEMBL4286963 | — | — | 1 | 5.87 |
| CHEMBL4283198 | — | — | 1 | 5.82 |
| CHEMBL4284799 | — | — | 1 | 5.80 |
| CHEMBL4286562 | — | — | 1 | 5.23 |
| CHEMBL4282878 | — | — | 1 | 5.21 |
| CHEMBL4276860 | — | — | 1 | - |
| CHEMBL4280294 | — | — | 1 | - |
| CHEMBL4290377 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4277610 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4285555 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4277193 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4288086 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4281035 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4292320 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4280180 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4287845 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4279720 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4292341 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4293778 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4288935 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL4294868 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4281393 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL4281693 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4284396 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL4278647 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL4292010 | — | IC50 | = | 711.0 | nM | 6.15 |
| CHEMBL4284952 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL4288201 | — | IC50 | = | 1211.0 | nM | 5.92 |
| CHEMBL4292612 | — | IC50 | = | 1226.0 | nM | 5.91 |
| CHEMBL4286963 | — | IC50 | = | 1338.0 | nM | 5.87 |
| CHEMBL4283198 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4284799 | — | IC50 | = | 1592.0 | nM | 5.80 |
| CHEMBL4286562 | — | IC50 | = | 5828.0 | nM | 5.23 |
| CHEMBL4282878 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL4276860 | — | IC50 | > | 5820.0 | nM | - |
| CHEMBL4280294 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4290377 | — | IC50 | - | — | - |