Assay Detail
Binding
CHEMBL3794752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged FLT3 cytoplasmic domain (564 to 993 residues) expressed in baculovirus expression system using 5-FAM-peptide 2 as substrate after 2 hrs by electrophoretic mobility shift assay in presence of ATP
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.93 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3792850 | — | — | 1 | 8.00 |
| CHEMBL3793843 | — | — | 1 | 7.47 |
| CHEMBL3793804 | — | — | 1 | 7.38 |
| CHEMBL3793847 | — | — | 1 | 7.37 |
| CHEMBL3793427 | — | — | 1 | 7.34 |
| CHEMBL3792973 | — | — | 1 | 7.25 |
| CHEMBL3794211 | — | — | 1 | 7.21 |
| CHEMBL3793695 | — | — | 1 | 7.05 |
| CHEMBL3792878 | — | — | 1 | 7.02 |
| CHEMBL3792955 | — | — | 1 | 6.97 |
| CHEMBL3793933 | — | — | 1 | 6.96 |
| CHEMBL3794503 | — | — | 1 | 6.95 |
| CHEMBL3794507 | — | — | 1 | 6.55 |
| CHEMBL3794415 | — | — | 1 | 6.51 |
| CHEMBL1288651 | — | — | 1 | 6.45 |
| CHEMBL508964 | — | — | 1 | 6.38 |
| CHEMBL3793590 | — | — | 1 | 6.35 |
| CHEMBL3792695 | — | — | 1 | 6.26 |
| CHEMBL3793337 | — | — | 1 | 6.11 |
| CHEMBL3793334 | — | — | 1 | - |
| CHEMBL3792732 | — | — | 1 | - |
| CHEMBL3794579 | — | — | 1 | - |
| CHEMBL3793040 | — | — | 1 | - |
| CHEMBL3794143 | — | — | 1 | - |
| CHEMBL3792669 | — | — | 1 | - |
| CHEMBL3792750 | — | — | 1 | - |
| CHEMBL3792787 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3792850 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3793843 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3793804 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3793847 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3793427 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3792973 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3794211 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3793695 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3792878 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3792955 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3793933 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3794503 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3794507 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3794415 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1288651 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL508964 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL3793590 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL3792695 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL3793337 | — | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL3793334 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3792732 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3794579 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3793040 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3794143 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3792669 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3792750 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3792787 | — | IC50 | > | 2000.0 | nM | - |