Assay Detail
Binding
CHEMBL5738871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HotSpot Assay: Table 3 and 4: The HotSpot kinase profiling and screening assays were carried out using the method of Anastassiadis et al., Nat. Biotechnol. (2011) Vol. 29, No. 11, pp. 1039-1045 (which is herein incorporated by reference in its entirety); 10 uM was the starting concentration with a 3-fold series dilution (10 doses) and the final ATP concentration was 10 uM.
36
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.28 | 7.68 |
| kon | 12 | - | - |
| k_off | 12 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | 4.0 | 6 | 7.68 |
| CHEMBL256961 | — | — | 3 | 7.39 |
| CHEMBL256570 | — | — | 6 | 6.98 |
| CHEMBL3683258 | — | — | 6 | 6.98 |
| CHEMBL5927784 | — | — | 6 | - |
| CHEMBL6002371 | — | — | 6 | - |
| CHEMBL5949720 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL256961 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL256570 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3683258 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL256570 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5949720 | — | k_off | = | - | s-1 | - |
| CHEMBL256570 | — | kon | = | - | — | - |
| CHEMBL5949720 | — | kon | = | - | — | - |
| CHEMBL5949720 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL256961 | — | k_off | = | - | s-1 | - |
| CHEMBL256961 | — | kon | = | - | — | - |
| CHEMBL576982 | QUIZARTINIB | k_off | = | - | s-1 | - |
| CHEMBL576982 | QUIZARTINIB | kon | = | - | — | - |
| CHEMBL6002371 | — | k_off | = | - | s-1 | - |
| CHEMBL6002371 | — | kon | = | - | — | - |
| CHEMBL6002371 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL5927784 | — | k_off | = | - | s-1 | - |
| CHEMBL5927784 | — | kon | = | - | — | - |
| CHEMBL5927784 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL256570 | — | k_off | = | - | s-1 | - |
| CHEMBL6002371 | — | kon | = | - | — | - |
| CHEMBL3683258 | — | k_off | = | - | s-1 | - |
| CHEMBL3683258 | — | kon | = | - | — | - |
| CHEMBL256570 | — | k_off | = | - | s-1 | - |
| CHEMBL256570 | — | kon | = | - | — | - |
| CHEMBL576982 | QUIZARTINIB | k_off | = | - | s-1 | - |
| CHEMBL576982 | QUIZARTINIB | kon | = | - | — | - |
| CHEMBL3683258 | — | k_off | = | - | s-1 | - |
| CHEMBL3683258 | — | kon | = | - | — | - |
| CHEMBL3683258 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL5927784 | — | k_off | = | - | s-1 | - |
| CHEMBL5927784 | — | kon | = | - | — | - |
| CHEMBL5927784 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL6002371 | — | IC50 | < | 0.508 | nM | - |
| CHEMBL6002371 | — | k_off | = | - | s-1 | - |