Assay Detail
Binding
CHEMBL4347596
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Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay
27
Total Activities
27
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
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.76 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453646 | — | — | 1 | 8.70 |
| CHEMBL4526274 | — | — | 1 | 8.40 |
| CHEMBL4564021 | — | — | 1 | 8.30 |
| CHEMBL4466059 | — | — | 1 | 8.30 |
| CHEMBL4462229 | — | — | 1 | 8.15 |
| CHEMBL4549369 | — | — | 1 | 8.00 |
| CHEMBL4457617 | — | — | 1 | 8.00 |
| CHEMBL4471710 | — | — | 1 | 8.00 |
| CHEMBL4443462 | — | — | 1 | 7.92 |
| CHEMBL4575813 | — | — | 1 | 7.85 |
| CHEMBL4520721 | — | — | 1 | 7.82 |
| CHEMBL4559926 | — | — | 1 | 7.75 |
| CHEMBL4556463 | — | — | 1 | 7.70 |
| CHEMBL4563723 | — | — | 1 | 7.68 |
| CHEMBL4592912 | — | — | 1 | 7.66 |
| CHEMBL4469297 | — | — | 1 | 7.52 |
| CHEMBL4451298 | — | — | 1 | 7.44 |
| CHEMBL4575735 | — | — | 1 | 7.44 |
| CHEMBL4540416 | — | — | 1 | 7.37 |
| CHEMBL4533614 | — | — | 1 | 7.34 |
| CHEMBL4568644 | — | — | 1 | 7.34 |
| CHEMBL4562491 | — | — | 1 | 7.30 |
| CHEMBL4584008 | — | — | 1 | 7.21 |
| CHEMBL4439450 | — | — | 1 | 7.07 |
| CHEMBL4441124 | — | — | 1 | - |
| CHEMBL4538220 | — | — | 1 | - |
| CHEMBL4581017 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453646 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4526274 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4564021 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4466059 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4462229 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4549369 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4457617 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4471710 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4443462 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4575813 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4520721 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4559926 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4556463 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4563723 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4592912 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4469297 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4451298 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4575735 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4540416 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4533614 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4568644 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4562491 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4584008 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4439450 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4441124 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4538220 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4581017 | — | IC50 | > | 100.0 | nM | - |