Assay Detail
Binding
CHEMBL4059185
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CDK2/Cyclin A1 using histone H1 as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition measure after 120 mins by filter binding method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 8.07 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4080236 | — | — | 1 | 8.97 |
| CHEMBL4093906 | — | — | 1 | 8.80 |
| CHEMBL4073053 | — | — | 1 | 8.76 |
| CHEMBL4086149 | — | — | 1 | 8.73 |
| CHEMBL4093755 | — | — | 1 | 8.72 |
| CHEMBL4076277 | — | — | 1 | 8.69 |
| CHEMBL4104057 | — | — | 1 | 8.68 |
| CHEMBL4077071 | — | — | 1 | 8.61 |
| CHEMBL4101635 | — | — | 1 | 8.52 |
| CHEMBL4075723 | — | — | 1 | 8.48 |
| CHEMBL4077074 | — | — | 1 | 8.47 |
| CHEMBL4096307 | — | — | 1 | 8.41 |
| CHEMBL4078261 | — | — | 1 | 8.35 |
| CHEMBL4074948 | — | — | 1 | 8.35 |
| CHEMBL4088753 | — | — | 1 | 8.28 |
| CHEMBL4067804 | — | — | 1 | 8.24 |
| CHEMBL4075720 | — | — | 1 | 8.23 |
| CHEMBL4103390 | — | — | 1 | 8.14 |
| CHEMBL4073283 | — | — | 1 | 8.13 |
| CHEMBL4071450 | — | — | 1 | 8.08 |
| CHEMBL4061686 | — | — | 1 | 8.03 |
| CHEMBL4099013 | — | — | 1 | 8.01 |
| CHEMBL4077278 | — | — | 1 | 7.93 |
| CHEMBL4092761 | — | — | 1 | 7.87 |
| CHEMBL4103338 | — | — | 1 | 7.78 |
| CHEMBL4064843 | — | — | 1 | 7.62 |
| CHEMBL4075466 | — | — | 1 | 7.53 |
| CHEMBL4098796 | — | — | 1 | 7.24 |
| CHEMBL4059849 | — | — | 1 | 7.23 |
| CHEMBL4075982 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4080236 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL4093906 | — | IC50 | = | 1.59 | nM | 8.80 |
| CHEMBL4073053 | — | IC50 | = | 1.74 | nM | 8.76 |
| CHEMBL4086149 | — | IC50 | = | 1.87 | nM | 8.73 |
| CHEMBL4093755 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4076277 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL4104057 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL4077071 | — | IC50 | = | 2.47 | nM | 8.61 |
| CHEMBL4101635 | — | IC50 | = | 3.03 | nM | 8.52 |
| CHEMBL4075723 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4077074 | — | IC50 | = | 3.36 | nM | 8.47 |
| CHEMBL4096307 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL4078261 | — | IC50 | = | 4.49 | nM | 8.35 |
| CHEMBL4074948 | — | IC50 | = | 4.49 | nM | 8.35 |
| CHEMBL4088753 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4067804 | — | IC50 | = | 5.74 | nM | 8.24 |
| CHEMBL4075720 | — | IC50 | = | 5.85 | nM | 8.23 |
| CHEMBL4103390 | — | IC50 | = | 7.25 | nM | 8.14 |
| CHEMBL4073283 | — | IC50 | = | 7.34 | nM | 8.13 |
| CHEMBL4071450 | — | IC50 | = | 8.27 | nM | 8.08 |
| CHEMBL4061686 | — | IC50 | = | 9.32 | nM | 8.03 |
| CHEMBL4099013 | — | IC50 | = | 9.85 | nM | 8.01 |
| CHEMBL4077278 | — | IC50 | = | 11.64 | nM | 7.93 |
| CHEMBL4092761 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4103338 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL4064843 | — | IC50 | = | 24.15 | nM | 7.62 |
| CHEMBL4075466 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4098796 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL4059849 | — | IC50 | = | 58.63 | nM | 7.23 |
| CHEMBL4075982 | — | IC50 | = | 287.19 | nM | 6.54 |
| CHEMBL4078605 | — | IC50 | = | 318.21 | nM | 6.50 |
| CHEMBL4066619 | — | IC50 | = | 697.0 | nM | 6.16 |
| CHEMBL4088115 | — | IC50 | - | — | - | |
| CHEMBL4097755 | — | IC50 | - | — | - | |
| CHEMBL4061687 | — | IC50 | - | — | - | |
| CHEMBL1336 | SORAFENIB | IC50 | - | — | - | |
| CHEMBL4086011 | — | IC50 | - | — | - | |
| CHEMBL4076183 | — | IC50 | - | — | - | |
| CHEMBL4064488 | — | IC50 | - | — | - |