Assay Detail
Binding
CHEMBL5733745
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Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software.
63
Total Activities
21
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
Compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.64 | 7.26 |
| kon | 21 | - | - |
| k_off | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6018546 | — | — | 3 | 7.26 |
| CHEMBL5747601 | — | — | 3 | 7.26 |
| CHEMBL3823861 | — | — | 3 | 7.26 |
| CHEMBL3823692 | — | — | 3 | 6.26 |
| CHEMBL3823212 | — | — | 3 | 6.26 |
| CHEMBL3823255 | — | — | 3 | 6.26 |
| CHEMBL3824228 | — | — | 3 | 6.26 |
| CHEMBL3823711 | — | — | 3 | 6.26 |
| CHEMBL3823849 | — | — | 3 | - |
| CHEMBL3822591 | — | — | 3 | - |
| CHEMBL3823556 | — | — | 3 | - |
| CHEMBL3824089 | — | — | 3 | - |
| CHEMBL3824233 | — | — | 3 | - |
| CHEMBL3823104 | — | — | 3 | - |
| CHEMBL3823543 | — | — | 3 | - |
| CHEMBL3823620 | — | — | 3 | - |
| CHEMBL3824021 | — | — | 3 | - |
| CHEMBL3824116 | — | — | 3 | - |
| CHEMBL3824279 | — | — | 3 | - |
| CHEMBL3823606 | — | — | 3 | - |
| CHEMBL1421 | DASATINIB ANHYDROUS | 4.0 | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3823861 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5747601 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6018546 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3823255 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3823692 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3823212 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3823711 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3824228 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3823692 | — | k_off | = | - | s-1 | - |
| CHEMBL3824279 | — | kon | = | - | — | - |
| CHEMBL3823692 | — | kon | = | - | — | - |
| CHEMBL3823606 | — | k_off | = | - | s-1 | - |
| CHEMBL3823606 | — | kon | = | - | — | - |
| CHEMBL6018546 | — | kon | = | - | — | - |
| CHEMBL1421 | DASATINIB ANHYDROUS | k_off | = | - | s-1 | - |
| CHEMBL1421 | DASATINIB ANHYDROUS | kon | = | - | — | - |
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | < | 10.0 | nM | - |
| CHEMBL3824279 | — | k_off | = | - | s-1 | - |
| CHEMBL3823255 | — | kon | = | - | — | - |
| CHEMBL3823212 | — | kon | = | - | — | - |
| CHEMBL3823212 | — | k_off | = | - | s-1 | - |
| CHEMBL3823849 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3823849 | — | kon | = | - | — | - |
| CHEMBL3823849 | — | k_off | = | - | s-1 | - |
| CHEMBL3822591 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3822591 | — | kon | = | - | — | - |
| CHEMBL3822591 | — | k_off | = | - | s-1 | - |
| CHEMBL3823861 | — | kon | = | - | — | - |
| CHEMBL3823861 | — | k_off | = | - | s-1 | - |
| CHEMBL3823543 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3823620 | — | k_off | = | - | s-1 | - |
| CHEMBL3824021 | — | kon | = | - | — | - |
| CHEMBL3823620 | — | kon | = | - | — | - |
| CHEMBL3823620 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3824228 | — | k_off | = | - | s-1 | - |
| CHEMBL3824228 | — | kon | = | - | — | - |
| CHEMBL3823711 | — | k_off | = | - | s-1 | - |
| CHEMBL3823711 | — | kon | = | - | — | - |
| CHEMBL3823543 | — | k_off | = | - | s-1 | - |
| CHEMBL3823543 | — | kon | = | - | — | - |
| CHEMBL3824279 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3823255 | — | k_off | = | - | s-1 | - |
| CHEMBL3824021 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3823104 | — | kon | = | - | — | - |
| CHEMBL3824021 | — | k_off | = | - | s-1 | - |
| CHEMBL3824116 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL3824116 | — | kon | = | - | — | - |
| CHEMBL3824116 | — | k_off | = | - | s-1 | - |
| CHEMBL5747601 | — | kon | = | - | — | - |
| CHEMBL5747601 | — | k_off | = | - | s-1 | - |