Assay Detail
Binding
CHEMBL4406242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged JAK1 (866 to 1154 residues) expressed in insect cells using FITC-labeled C6-KKHTDDGYMPMSPGVA-NH peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay
21
Total Activities
21
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
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.13 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4446962 | — | — | 1 | 8.40 |
| CHEMBL4064366 | — | — | 1 | 8.15 |
| CHEMBL4577393 | — | — | 1 | 8.10 |
| CHEMBL4450982 | — | — | 1 | 8.00 |
| CHEMBL4441479 | — | — | 1 | 7.75 |
| CHEMBL4541637 | — | — | 1 | 7.72 |
| CHEMBL4544007 | — | — | 1 | 7.70 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.70 |
| CHEMBL4466590 | — | — | 1 | 7.57 |
| CHEMBL4536860 | — | — | 1 | 7.40 |
| CHEMBL4452410 | — | — | 1 | 7.37 |
| CHEMBL4577523 | GOLIDOCITINIB | 2.0 | 1 | 7.16 |
| CHEMBL4444782 | — | — | 1 | 7.16 |
| CHEMBL4449567 | — | — | 1 | 6.89 |
| CHEMBL4588587 | — | — | 1 | 6.75 |
| CHEMBL4466247 | — | — | 1 | 6.58 |
| CHEMBL4553035 | — | — | 1 | 6.34 |
| CHEMBL4551327 | — | — | 1 | 5.96 |
| CHEMBL4588128 | — | — | 1 | 5.77 |
| CHEMBL4517840 | — | — | 1 | 5.66 |
| CHEMBL4476801 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4446962 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4064366 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4577393 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4450982 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4441479 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4541637 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4544007 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4466590 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4536860 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4452410 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4577523 | GOLIDOCITINIB | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4444782 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4449567 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4588587 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4466247 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4553035 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4551327 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4588128 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4517840 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4476801 | — | IC50 | = | 2400.0 | nM | 5.62 |