Assay Detail
Binding
CHEMBL2329569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK1 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr by scintillation counting analysis in presence of [gamma-33P]ATP
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
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.24 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325897 | — | — | 1 | 9.33 |
| CHEMBL2325898 | — | — | 1 | 9.23 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.80 |
| CHEMBL2325895 | — | — | 1 | 8.49 |
| CHEMBL2325900 | — | — | 1 | 7.62 |
| CHEMBL2325912 | — | — | 1 | 7.35 |
| CHEMBL2325899 | — | — | 1 | 7.35 |
| CHEMBL2325903 | — | — | 1 | 7.35 |
| CHEMBL2325894 | — | — | 1 | 7.33 |
| CHEMBL2325902 | — | — | 1 | 7.12 |
| CHEMBL2325905 | — | — | 1 | 7.00 |
| CHEMBL2325906 | — | — | 1 | 6.97 |
| CHEMBL2325901 | — | — | 1 | 6.65 |
| CHEMBL2325904 | — | — | 1 | 6.59 |
| CHEMBL2325913 | — | — | 1 | 6.57 |
| CHEMBL2325909 | — | — | 1 | 6.44 |
| CHEMBL2325910 | — | — | 1 | 6.37 |
| CHEMBL2325908 | — | — | 1 | 6.20 |
| CHEMBL2325911 | — | — | 1 | 6.06 |
| CHEMBL2325907 | — | — | 1 | 5.96 |
| CHEMBL2325896 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325897 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2325898 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2325895 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL2325900 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2325912 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL2325899 | — | IC50 | = | 44.8 | nM | 7.35 |
| CHEMBL2325903 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL2325894 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2325902 | — | IC50 | = | 75.8 | nM | 7.12 |
| CHEMBL2325905 | — | IC50 | = | 99.7 | nM | 7.00 |
| CHEMBL2325906 | — | IC50 | = | 108.1 | nM | 6.97 |
| CHEMBL2325901 | — | IC50 | = | 224.3 | nM | 6.65 |
| CHEMBL2325904 | — | IC50 | = | 256.7 | nM | 6.59 |
| CHEMBL2325913 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL2325909 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL2325910 | — | IC50 | = | 430.5 | nM | 6.37 |
| CHEMBL2325908 | — | IC50 | = | 636.6 | nM | 6.20 |
| CHEMBL2325911 | — | IC50 | = | 870.7 | nM | 6.06 |
| CHEMBL2325907 | — | IC50 | = | 1102.5 | nM | 5.96 |
| CHEMBL2325896 | — | IC50 | < | 0.5 | nM | - |