Assay Detail
Binding
CHEMBL4265552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged JAK3 JH1 domain using KAIETDKEYYTVKD-NH2 as substrate in presence of ATP at Km 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 | 8.36 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085457 | RITLECITINIB | 4.0 | 1 | 9.52 |
| CHEMBL4280180 | — | — | 1 | 9.30 |
| CHEMBL4292341 | — | — | 1 | 9.30 |
| CHEMBL4288086 | — | — | 1 | 9.30 |
| CHEMBL4279720 | — | — | 1 | 9.15 |
| CHEMBL4287845 | — | — | 1 | 9.15 |
| CHEMBL4292320 | — | — | 1 | 9.05 |
| CHEMBL4288935 | — | — | 1 | 9.00 |
| CHEMBL4293778 | — | — | 1 | 9.00 |
| CHEMBL4294868 | — | — | 1 | 9.00 |
| CHEMBL4281693 | — | — | 1 | 8.70 |
| CHEMBL4284396 | — | — | 1 | 8.52 |
| CHEMBL4281393 | — | — | 1 | 8.52 |
| CHEMBL4292010 | — | — | 1 | 8.22 |
| CHEMBL4278647 | — | — | 1 | 8.22 |
| CHEMBL4288201 | — | — | 1 | 8.15 |
| CHEMBL4284952 | — | — | 1 | 8.15 |
| CHEMBL4284799 | — | — | 1 | 7.92 |
| CHEMBL4286963 | — | — | 1 | 7.89 |
| CHEMBL4283198 | — | — | 1 | 7.89 |
| CHEMBL4292612 | — | — | 1 | 7.77 |
| CHEMBL4282878 | — | — | 1 | 7.58 |
| CHEMBL4286562 | — | — | 1 | 7.31 |
| CHEMBL4276860 | — | — | 1 | 7.18 |
| CHEMBL4290377 | — | — | 1 | 6.92 |
| CHEMBL4280294 | — | — | 1 | 6.64 |
| CHEMBL4281035 | — | — | 1 | - |
| CHEMBL4285555 | — | — | 1 | - |
| CHEMBL4277610 | — | — | 1 | - |
| CHEMBL4277193 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085457 | RITLECITINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4280180 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4292341 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4288086 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4279720 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4287845 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4292320 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4288935 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4293778 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4294868 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4281693 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4284396 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4281393 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4292010 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4278647 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4288201 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4284952 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4284799 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4286963 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4283198 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4292612 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4282878 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4286562 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4276860 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4290377 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4280294 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4281035 | — | IC50 | - | — | - | |
| CHEMBL4285555 | — | IC50 | - | — | - | |
| CHEMBL4277610 | — | IC50 | - | — | - | |
| CHEMBL4277193 | — | IC50 | - | — | - |