Assay Detail
Functional
CHEMBL3877424
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Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEL 92.1.7 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.09 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.31 |
| CHEMBL3917405 | — | — | 1 | 6.03 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.93 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | - |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | - |
| CHEMBL3933593 | — | — | 1 | - |
| CHEMBL3972157 | — | — | 1 | - |
| CHEMBL3951291 | — | — | 1 | - |
| CHEMBL3945293 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3917405 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2035187 | PACRITINIB | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | > | 2000.0 | nM | - |
| CHEMBL1789941 | RUXOLITINIB | IC50 | > | 4000.0 | nM | - |
| CHEMBL3933593 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3972157 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3951291 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3945293 | — | IC50 | > | 2000.0 | nM | - |