Assay Detail
Binding
CHEMBL1926252
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Inhibition of human recombinant JAK2 using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate after 20 mins by fluorescence assay
31
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
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 9.05 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1822515 | — | — | 2 | 9.77 |
| CHEMBL1923571 | — | — | 1 | 9.77 |
| CHEMBL1923573 | — | — | 1 | 9.64 |
| CHEMBL1923588 | — | — | 1 | 9.52 |
| CHEMBL1923585 | — | — | 1 | 9.48 |
| CHEMBL1923575 | — | — | 1 | 9.46 |
| CHEMBL1923583 | — | — | 1 | 9.46 |
| CHEMBL1923580 | — | — | 1 | 9.44 |
| CHEMBL1923589 | — | — | 1 | 9.40 |
| CHEMBL1923590 | — | — | 1 | 9.40 |
| CHEMBL1923574 | — | — | 1 | 9.33 |
| CHEMBL1923579 | — | — | 1 | 9.30 |
| CHEMBL1923570 | — | — | 1 | 9.30 |
| CHEMBL1923584 | — | — | 1 | 9.30 |
| CHEMBL1923594 | — | — | 1 | 9.30 |
| CHEMBL1923577 | — | — | 1 | 9.27 |
| CHEMBL1923593 | — | — | 1 | 9.22 |
| CHEMBL1923576 | — | — | 1 | 9.10 |
| CHEMBL1923592 | — | — | 1 | 9.05 |
| CHEMBL1923586 | — | — | 1 | 9.00 |
| CHEMBL1923578 | — | — | 1 | 9.00 |
| CHEMBL1923582 | — | — | 1 | 8.96 |
| CHEMBL1923569 | — | — | 1 | 8.94 |
| CHEMBL1923587 | — | — | 1 | 8.92 |
| CHEMBL1921819 | — | — | 1 | 8.82 |
| CHEMBL1821735 | — | — | 1 | 8.80 |
| CHEMBL1923572 | — | — | 1 | 8.68 |
| CHEMBL1923581 | — | — | 1 | 8.43 |
| CHEMBL1822525 | — | — | 1 | 6.42 |
| CHEMBL1923591 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1923571 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1822515 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1822515 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL1923573 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL1923588 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1923585 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL1923583 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL1923575 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL1923580 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL1923589 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1923590 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1923574 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL1923594 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1923570 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1923579 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1923584 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1923577 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL1923593 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1923576 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1923592 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1923586 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1923578 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1923582 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1923569 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL1923587 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1921819 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1821735 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1923572 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1923581 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1822525 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL1923591 | — | IC50 | = | 480.0 | nM | 6.32 |