Assay Detail
Functional
CHEMBL4268249
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Antiproliferative activity against human KMS-12-BM cells after 72 hrs by MTT assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KMS-12-BM |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.26 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290748 | — | — | 1 | 7.16 |
| CHEMBL4283921 | — | — | 1 | 7.00 |
| CHEMBL4280540 | — | — | 1 | 6.70 |
| CHEMBL4294153 | — | — | 1 | 6.46 |
| CHEMBL4290689 | — | — | 1 | 6.27 |
| CHEMBL4278591 | — | — | 1 | 6.17 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.03 |
| CHEMBL4290831 | — | — | 1 | 5.94 |
| CHEMBL4291781 | — | — | 1 | 5.71 |
| CHEMBL4095596 | — | — | 1 | 5.70 |
| CHEMBL3917405 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290748 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4283921 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4280540 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4294153 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4290689 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4278591 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4290831 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4291781 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL4095596 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL3917405 | — | IC50 | = | 2110.0 | nM | 5.68 |