Assay Detail
Binding
CHEMBL2214784
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Inhibition of JAK2 in HEL 92.1.7 cells assessed as inhibition of STAT3 phosphorylation
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.03 | 6.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2208028 | — | — | 1 | 6.35 |
| CHEMBL2208032 | — | — | 1 | 6.34 |
| CHEMBL2207764 | — | — | 1 | 6.30 |
| CHEMBL2208025 | — | — | 1 | 6.23 |
| CHEMBL2208034 | — | — | 1 | 6.16 |
| CHEMBL1077458 | — | — | 1 | 6.10 |
| CHEMBL2207759 | — | — | 1 | 5.98 |
| CHEMBL2208024 | — | — | 1 | 5.88 |
| CHEMBL2208033 | — | — | 1 | 5.86 |
| CHEMBL2208031 | — | — | 1 | 5.82 |
| CHEMBL2208023 | — | — | 1 | 5.71 |
| CHEMBL2207760 | — | — | 1 | 5.66 |
| CHEMBL2207758 | — | — | 1 | - |
| CHEMBL2208035 | — | — | 1 | - |
| CHEMBL2208030 | — | — | 1 | - |
| CHEMBL2208029 | — | — | 1 | - |
| CHEMBL2208027 | — | — | 1 | - |
| CHEMBL2208026 | — | — | 1 | - |
| CHEMBL2207767 | — | — | 1 | - |
| CHEMBL2207761 | — | — | 1 | - |
| CHEMBL2207762 | — | — | 1 | - |
| CHEMBL2207763 | — | — | 1 | - |
| CHEMBL2207766 | — | — | 1 | - |
| CHEMBL2207765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2208028 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL2208032 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL2207764 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL2208025 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL2208034 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL1077458 | — | IC50 | = | 795.0 | nM | 6.10 |
| CHEMBL2207759 | — | IC50 | = | 1051.0 | nM | 5.98 |
| CHEMBL2208024 | — | IC50 | = | 1328.0 | nM | 5.88 |
| CHEMBL2208033 | — | IC50 | = | 1391.0 | nM | 5.86 |
| CHEMBL2208031 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL2208023 | — | IC50 | = | 1971.0 | nM | 5.71 |
| CHEMBL2207760 | — | IC50 | = | 2166.0 | nM | 5.66 |
| CHEMBL2207758 | — | IC50 | - | — | - | |
| CHEMBL2208035 | — | IC50 | - | — | - | |
| CHEMBL2208030 | — | IC50 | - | — | - | |
| CHEMBL2208029 | — | IC50 | - | — | - | |
| CHEMBL2208027 | — | IC50 | - | — | - | |
| CHEMBL2208026 | — | IC50 | - | — | - | |
| CHEMBL2207767 | — | IC50 | - | — | - | |
| CHEMBL2207761 | — | IC50 | - | — | - | |
| CHEMBL2207762 | — | IC50 | - | — | - | |
| CHEMBL2207763 | — | IC50 | - | — | - | |
| CHEMBL2207766 | — | IC50 | - | — | - | |
| CHEMBL2207765 | — | IC50 | - | — | - |