Assay Detail
Binding
CHEMBL4429476
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed by baculovirus in Sf21 insect cells measured after 10 mins in presence of [gamma-33P]ATP by scintillation counter method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.44 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4444648 | — | — | 1 | 8.70 |
| CHEMBL4519741 | — | — | 1 | 8.30 |
| CHEMBL4448466 | — | — | 1 | 8.22 |
| CHEMBL4514229 | — | — | 1 | 8.22 |
| CHEMBL4435299 | — | — | 1 | 8.10 |
| CHEMBL4435097 | — | — | 1 | 8.10 |
| CHEMBL4469122 | — | — | 1 | 8.00 |
| CHEMBL4519896 | — | — | 1 | 7.96 |
| CHEMBL4528431 | — | — | 1 | 7.57 |
| CHEMBL4460440 | — | — | 1 | 7.55 |
| CHEMBL4475895 | — | — | 1 | 7.44 |
| CHEMBL4440184 | — | — | 1 | 7.42 |
| CHEMBL2332840 | — | — | 1 | 7.41 |
| CHEMBL4444689 | — | — | 1 | 7.38 |
| CHEMBL4523041 | — | — | 1 | 7.30 |
| CHEMBL4591330 | — | — | 1 | 7.28 |
| CHEMBL4438387 | — | — | 1 | 7.28 |
| CHEMBL4451381 | — | — | 1 | 7.25 |
| CHEMBL4470513 | — | — | 1 | 7.21 |
| CHEMBL4474529 | — | — | 1 | 7.18 |
| CHEMBL4443351 | — | — | 1 | 7.14 |
| CHEMBL4471087 | — | — | 1 | 7.10 |
| CHEMBL4550097 | — | — | 1 | 7.09 |
| CHEMBL4544397 | — | — | 1 | 6.66 |
| CHEMBL4435018 | — | — | 1 | 6.53 |
| CHEMBL4530061 | — | — | 1 | 6.35 |
| CHEMBL4475159 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4444648 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4519741 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4448466 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4514229 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4435299 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4435097 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4469122 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4519896 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4528431 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4460440 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4475895 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4440184 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2332840 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4444689 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4523041 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4591330 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4438387 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4451381 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4470513 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4474529 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4443351 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4471087 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4550097 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4544397 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL4435018 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL4530061 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL4475159 | — | IC50 | = | 657.0 | nM | 6.18 |