Assay Detail
Binding
CHEMBL4406248
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Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| 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 | 7 | 6.97 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4064366 | — | — | 1 | 7.22 |
| CHEMBL4466590 | — | — | 1 | 7.10 |
| CHEMBL4577393 | — | — | 1 | 7.03 |
| CHEMBL4541637 | — | — | 1 | 6.92 |
| CHEMBL4450982 | — | — | 1 | 6.89 |
| CHEMBL4577523 | GOLIDOCITINIB | 2.0 | 1 | 6.89 |
| CHEMBL4449567 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4064366 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4466590 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4577393 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4541637 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4450982 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4577523 | GOLIDOCITINIB | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4449567 | — | IC50 | = | 180.0 | nM | 6.75 |