Assay Detail
Binding
CHEMBL4059187
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FLT3 using EAIYAAPFAKKK 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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.69 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4086149 | — | — | 1 | 10.00 |
| CHEMBL4092761 | — | — | 1 | 9.89 |
| CHEMBL4078261 | — | — | 1 | 9.78 |
| CHEMBL4077071 | — | — | 1 | 9.57 |
| CHEMBL4101635 | — | — | 1 | 9.49 |
| CHEMBL4104057 | — | — | 1 | 9.47 |
| CHEMBL4073053 | — | — | 1 | 9.42 |
| CHEMBL4075720 | — | — | 1 | 9.36 |
| CHEMBL4061686 | — | — | 1 | 9.33 |
| CHEMBL4093755 | — | — | 1 | 9.24 |
| CHEMBL4088753 | — | — | 1 | 9.23 |
| CHEMBL4077074 | — | — | 1 | 9.21 |
| CHEMBL4059849 | — | — | 1 | 9.02 |
| CHEMBL4074948 | — | — | 1 | 8.99 |
| CHEMBL4076277 | — | — | 1 | 8.98 |
| CHEMBL4080236 | — | — | 1 | 8.86 |
| CHEMBL4075723 | — | — | 1 | 8.81 |
| CHEMBL4103390 | — | — | 1 | 8.69 |
| CHEMBL4096307 | — | — | 1 | 8.64 |
| CHEMBL4103338 | — | — | 1 | 8.59 |
| CHEMBL4071450 | — | — | 1 | 8.50 |
| CHEMBL4073283 | — | — | 1 | 8.45 |
| CHEMBL4075466 | — | — | 1 | 8.42 |
| CHEMBL4067804 | — | — | 1 | 8.31 |
| CHEMBL4093906 | — | — | 1 | 8.27 |
| CHEMBL4077278 | — | — | 1 | 8.21 |
| CHEMBL4099013 | — | — | 1 | 8.12 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.81 |
| CHEMBL4064843 | — | — | 1 | 7.77 |
| CHEMBL4075982 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4086149 | — | IC50 | = | 0.101 | nM | 10.00 |
| CHEMBL4092761 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4078261 | — | IC50 | = | 0.167 | nM | 9.78 |
| CHEMBL4077071 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL4101635 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4104057 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4073053 | — | IC50 | = | 0.384 | nM | 9.42 |
| CHEMBL4075720 | — | IC50 | = | 0.438 | nM | 9.36 |
| CHEMBL4061686 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL4093755 | — | IC50 | = | 0.576 | nM | 9.24 |
| CHEMBL4088753 | — | IC50 | = | 0.588 | nM | 9.23 |
| CHEMBL4077074 | — | IC50 | = | 0.623 | nM | 9.21 |
| CHEMBL4059849 | — | IC50 | = | 0.958 | nM | 9.02 |
| CHEMBL4074948 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL4076277 | — | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4080236 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL4075723 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL4103390 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL4096307 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL4103338 | — | IC50 | = | 2.56 | nM | 8.59 |
| CHEMBL4071450 | — | IC50 | = | 3.17 | nM | 8.50 |
| CHEMBL4073283 | — | IC50 | = | 3.52 | nM | 8.45 |
| CHEMBL4075466 | — | IC50 | = | 3.78 | nM | 8.42 |
| CHEMBL4067804 | — | IC50 | = | 4.84 | nM | 8.31 |
| CHEMBL4093906 | — | IC50 | = | 5.36 | nM | 8.27 |
| CHEMBL4077278 | — | IC50 | = | 6.15 | nM | 8.21 |
| CHEMBL4099013 | — | IC50 | = | 7.63 | nM | 8.12 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 15.48 | nM | 7.81 |
| CHEMBL4064843 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL4075982 | — | IC50 | = | 42.38 | nM | 7.37 |
| CHEMBL4078605 | — | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL4061687 | — | IC50 | = | 97.4 | nM | 7.01 |
| CHEMBL4066619 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4076183 | — | IC50 | - | — | - | |
| CHEMBL4098796 | — | IC50 | - | — | - | |
| CHEMBL4088115 | — | IC50 | - | — | - | |
| CHEMBL4064488 | — | IC50 | - | — | - | |
| CHEMBL4086011 | — | IC50 | - | — | - | |
| CHEMBL4097755 | — | IC50 | - | — | - |