Assay Detail
Binding
CHEMBL2390018
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Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386796 | — | — | 1 | 8.70 |
| CHEMBL2386803 | — | — | 1 | 8.40 |
| CHEMBL2386788 | — | — | 1 | 8.22 |
| CHEMBL2386794 | — | — | 1 | 8.10 |
| CHEMBL2386790 | — | — | 1 | 8.05 |
| CHEMBL2386797 | — | — | 1 | 8.05 |
| CHEMBL2063324 | — | — | 1 | 8.00 |
| CHEMBL1807392 | — | — | 1 | 7.96 |
| CHEMBL2386812 | — | — | 1 | 7.89 |
| CHEMBL2386801 | — | — | 1 | 7.89 |
| CHEMBL2386792 | — | — | 1 | 7.82 |
| CHEMBL2386800 | — | — | 1 | 7.80 |
| CHEMBL2386807 | — | — | 1 | 7.77 |
| CHEMBL2386802 | — | — | 1 | 7.75 |
| CHEMBL2386793 | — | — | 1 | 7.72 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.70 |
| CHEMBL2386795 | — | — | 1 | 7.70 |
| CHEMBL2386805 | — | — | 1 | 7.68 |
| CHEMBL2386798 | — | — | 1 | 7.66 |
| CHEMBL2386809 | — | — | 1 | 7.58 |
| CHEMBL2386810 | — | — | 1 | 7.58 |
| CHEMBL2386789 | — | — | 1 | 7.52 |
| CHEMBL2386806 | — | — | 1 | 7.46 |
| CHEMBL2386816 | — | — | 1 | 7.40 |
| CHEMBL2386818 | — | — | 1 | 7.30 |
| CHEMBL2386814 | — | — | 1 | 7.28 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.27 |
| CHEMBL2386799 | — | — | 1 | 7.18 |
| CHEMBL2105709 | QUIZARTINIB DIHYDROCHLORIDE | 4.0 | 1 | 7.16 |
| CHEMBL2386815 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386796 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2386803 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2386788 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2386794 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2386790 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2386797 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2063324 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1807392 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2386812 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2386801 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2386792 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2386800 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2386807 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2386802 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2386793 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2386795 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2386805 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2386798 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2386809 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2386810 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2386789 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2386806 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2386816 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2386818 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2386814 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2386799 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2105709 | QUIZARTINIB DIHYDROCHLORIDE | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2386815 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2386817 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2386813 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2386808 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2386804 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2386791 | — | IC50 | = | 390.0 | nM | 6.41 |