Assay Detail
Binding
CHEMBL4265556
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Inhibition of recombinant human GST-tagged JAK2 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 | 5.91 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4279720 | — | — | 1 | 7.15 |
| CHEMBL4293778 | — | — | 1 | 7.01 |
| CHEMBL4282878 | — | — | 1 | 6.33 |
| CHEMBL4288201 | — | — | 1 | 6.11 |
| CHEMBL4284952 | — | — | 1 | 6.06 |
| CHEMBL4278647 | — | — | 1 | 5.98 |
| CHEMBL4276860 | — | — | 1 | 5.95 |
| CHEMBL4292010 | — | — | 1 | 5.81 |
| CHEMBL4281393 | — | — | 1 | 5.78 |
| CHEMBL4283198 | — | — | 1 | 5.73 |
| CHEMBL4285555 | — | — | 1 | 5.62 |
| CHEMBL4286963 | — | — | 1 | 5.61 |
| CHEMBL4277193 | — | — | 1 | 5.59 |
| CHEMBL4277610 | — | — | 1 | 5.52 |
| CHEMBL4281693 | — | — | 1 | 5.30 |
| CHEMBL4280294 | — | — | 1 | 5.06 |
| CHEMBL4286562 | — | — | 1 | - |
| CHEMBL4281035 | — | — | 1 | - |
| CHEMBL4287845 | — | — | 1 | - |
| CHEMBL4292341 | — | — | 1 | - |
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | - |
| CHEMBL4288086 | — | — | 1 | - |
| CHEMBL4288935 | — | — | 1 | - |
| CHEMBL4292320 | — | — | 1 | - |
| CHEMBL4294868 | — | — | 1 | - |
| CHEMBL4290377 | — | — | 1 | - |
| CHEMBL4284799 | — | — | 1 | - |
| CHEMBL4284396 | — | — | 1 | - |
| CHEMBL4292612 | — | — | 1 | - |
| CHEMBL4280180 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4279720 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4293778 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4282878 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4288201 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL4284952 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL4278647 | — | IC50 | = | 1046.0 | nM | 5.98 |
| CHEMBL4276860 | — | IC50 | = | 1118.0 | nM | 5.95 |
| CHEMBL4292010 | — | IC50 | = | 1544.0 | nM | 5.81 |
| CHEMBL4281393 | — | IC50 | = | 1666.0 | nM | 5.78 |
| CHEMBL4283198 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL4285555 | — | IC50 | = | 2419.0 | nM | 5.62 |
| CHEMBL4286963 | — | IC50 | = | 2455.0 | nM | 5.61 |
| CHEMBL4277193 | — | IC50 | = | 2554.0 | nM | 5.59 |
| CHEMBL4277610 | — | IC50 | = | 3012.0 | nM | 5.52 |
| CHEMBL4281693 | — | IC50 | = | 4964.0 | nM | 5.30 |
| CHEMBL4280294 | — | IC50 | = | 8623.0 | nM | 5.06 |
| CHEMBL4286562 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4281035 | — | IC50 | > | 7646.0 | nM | - |
| CHEMBL4287845 | — | IC50 | > | 6578.0 | nM | - |
| CHEMBL4292341 | — | IC50 | > | 9925.0 | nM | - |
| CHEMBL4085457 | RITLECITINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL4288086 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4288935 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4292320 | — | IC50 | > | 7448.0 | nM | - |
| CHEMBL4294868 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4290377 | — | IC50 | - | — | - | |
| CHEMBL4284799 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4284396 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4292612 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4280180 | — | IC50 | > | 10000.0 | nM | - |