Assay Detail
Binding
CHEMBL5738875
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.
99
Total Activities
29
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 33 | 7.16 | 8.71 |
| kon | 33 | - | - |
| k_off | 33 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | 4.0 | 6 | 8.71 |
| CHEMBL5949720 | — | — | 3 | 8.30 |
| CHEMBL5865662 | — | — | 3 | 8.22 |
| CHEMBL5931611 | — | — | 3 | 7.82 |
| CHEMBL5800402 | — | — | 3 | 7.82 |
| CHEMBL6012486 | — | — | 3 | 7.82 |
| CHEMBL256570 | — | — | 6 | 7.80 |
| CHEMBL256961 | — | — | 3 | 7.66 |
| CHEMBL6002371 | — | — | 6 | 7.58 |
| CHEMBL5917089 | — | — | 3 | 7.52 |
| CHEMBL401633 | — | — | 3 | 7.52 |
| CHEMBL5856678 | — | — | 3 | 7.47 |
| CHEMBL256963 | — | — | 3 | 7.35 |
| CHEMBL5760981 | — | — | 3 | 7.28 |
| CHEMBL5900939 | — | — | 3 | 7.17 |
| CHEMBL5760895 | — | — | 3 | 6.92 |
| CHEMBL5942885 | — | — | 3 | 6.85 |
| CHEMBL5968312 | — | — | 3 | 6.80 |
| CHEMBL5920310 | — | — | 3 | 6.78 |
| CHEMBL437208 | — | — | 3 | 6.58 |
| CHEMBL5941362 | — | — | 3 | 6.54 |
| CHEMBL6006619 | — | — | 3 | 6.53 |
| CHEMBL5820469 | — | — | 3 | 6.50 |
| CHEMBL5918176 | — | — | 3 | 6.42 |
| CHEMBL6045013 | — | — | 3 | 6.36 |
| CHEMBL5768844 | — | — | 3 | 6.05 |
| CHEMBL3182364 | — | — | 3 | 6.02 |
| CHEMBL6021522 | — | — | 3 | 6.01 |
| CHEMBL5927784 | — | — | 6 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL5949720 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5865662 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5931611 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5800402 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6012486 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL256570 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL256961 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL6002371 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5917089 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL401633 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5856678 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL256963 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5760981 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5900939 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5760895 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5942885 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5968312 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5920310 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL437208 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5941362 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL6006619 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL5820469 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL5918176 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL6045013 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL5768844 | — | IC50 | = | 892.0 | nM | 6.05 |
| CHEMBL3182364 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL6021522 | — | IC50 | = | 973.0 | nM | 6.01 |
| CHEMBL5931611 | — | kon | = | - | — | - |
| CHEMBL5942885 | — | k_off | = | - | s-1 | - |
| CHEMBL5920310 | — | kon | = | - | — | - |
| CHEMBL5920310 | — | k_off | = | - | s-1 | - |
| CHEMBL6006619 | — | kon | = | - | — | - |
| CHEMBL6006619 | — | k_off | = | - | s-1 | - |
| CHEMBL5900939 | — | kon | = | - | — | - |
| CHEMBL5900939 | — | k_off | = | - | s-1 | - |
| CHEMBL576982 | QUIZARTINIB | IC50 | < | 5.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | kon | = | - | — | - |
| CHEMBL576982 | QUIZARTINIB | k_off | = | - | s-1 | - |
| CHEMBL5931611 | — | k_off | = | - | s-1 | - |
| CHEMBL5927784 | — | kon | = | - | — | - |
| CHEMBL6002371 | — | k_off | = | - | s-1 | - |
| CHEMBL5800402 | — | k_off | = | - | s-1 | - |
| CHEMBL5927784 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL6002371 | — | kon | = | - | — | - |
| CHEMBL6012486 | — | kon | = | - | — | - |
| CHEMBL5927784 | — | k_off | = | - | s-1 | - |
| CHEMBL5949720 | — | k_off | = | - | s-1 | - |
| CHEMBL5942885 | — | kon | = | - | — | - |
| CHEMBL6012486 | — | k_off | = | - | s-1 | - |