Assay Detail
Binding
CHEMBL5738884
Review assay metadata, readout intent, target linkage, and publication context from the same page.
IC50 Kinase Assays: Table 8-10: Compounds were tested in 10-dose IC50 mode with 3-fold serial dilution starting at 10 uM, and are relative to DMSO, the negative control. The positive control, Staurosporine, was tested in a 10-dose IC50 mode with 4-fold serial dilution starting at 20 uM. Reactions were carried out at 10 uM ATP. Curve fits were performed to determine IC50 where the enzyme activities at the highest concentration of compounds were less than 65%.
15
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 10.18 | 11.00 |
| kon | 5 | - | - |
| k_off | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5927784 | — | — | 3 | 11.00 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 3 | 10.80 |
| CHEMBL6002371 | — | — | 3 | 10.68 |
| CHEMBL256961 | — | — | 3 | 10.03 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 3 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5927784 | — | Kd | = | 0.01 | nM | 11.00 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 0.016 | nM | 10.80 |
| CHEMBL6002371 | — | Kd | = | 0.021 | nM | 10.68 |
| CHEMBL256961 | — | Kd | = | 0.093 | nM | 10.03 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 4.2 | nM | 8.38 |
| CHEMBL576982 | QUIZARTINIB | kon | = | - | — | - |
| CHEMBL576982 | QUIZARTINIB | k_off | = | - | s-1 | - |
| CHEMBL256961 | — | kon | = | - | — | - |
| CHEMBL256961 | — | k_off | = | - | s-1 | - |
| CHEMBL2105728 | CRENOLANIB | kon | = | - | — | - |
| CHEMBL2105728 | CRENOLANIB | k_off | = | - | s-1 | - |
| CHEMBL6002371 | — | kon | = | - | — | - |
| CHEMBL6002371 | — | k_off | = | - | s-1 | - |
| CHEMBL5927784 | — | kon | = | - | — | - |
| CHEMBL5927784 | — | k_off | = | - | s-1 | - |