Assay Detail
Binding
CHEMBL5733415
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The enzymatic activity of FLT3 was determined using the Z-Lyte assay kit from Invitrogen (Invitrogen cat #PV3191). The assay was performed using the recommended manufacturer's instructions with 117.5 uM ATP and 1 nM FLT3 (Invitrogen cat #PV3182). The % inhibition values were determined according to the manufacturer's directions and IC50 values were obtained using a non-linear 4 point logistic curve fit (XLfit4, IDBS).
90
Total Activities
30
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
Kinase inhibitors and method of treating cancer
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.26 | 6.26 |
| kon | 30 | - | - |
| k_off | 30 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5883690 | — | — | 3 | 6.26 |
| CHEMBL5953937 | — | — | 3 | 6.26 |
| CHEMBL6055889 | — | — | 3 | 6.26 |
| CHEMBL5766435 | — | — | 3 | 6.26 |
| CHEMBL6010893 | — | — | 3 | 6.26 |
| CHEMBL6030772 | — | — | 3 | 6.26 |
| CHEMBL4440053 | — | — | 3 | 6.26 |
| CHEMBL5927653 | — | — | 3 | 6.26 |
| CHEMBL5760570 | — | — | 3 | 6.26 |
| CHEMBL3408947 | OCIFISERTIB | 2.0 | 3 | 6.26 |
| CHEMBL3353347 | — | — | 3 | - |
| CHEMBL3353341 | — | — | 3 | - |
| CHEMBL4448596 | — | — | 3 | - |
| CHEMBL3353355 | — | — | 3 | - |
| CHEMBL5767225 | — | — | 3 | - |
| CHEMBL5982085 | — | — | 3 | - |
| CHEMBL5766613 | — | — | 3 | - |
| CHEMBL3353354 | — | — | 3 | - |
| CHEMBL3353362 | — | — | 3 | - |
| CHEMBL6042583 | — | — | 3 | - |
| CHEMBL4440812 | — | — | 3 | - |
| CHEMBL5873734 | — | — | 3 | - |
| CHEMBL4516793 | — | — | 3 | - |
| CHEMBL5814185 | — | — | 3 | - |
| CHEMBL5831336 | — | — | 3 | - |
| CHEMBL5867004 | — | — | 3 | - |
| CHEMBL5907354 | — | — | 3 | - |
| CHEMBL5797099 | — | — | 3 | - |
| CHEMBL6030782 | — | — | 3 | - |
| CHEMBL5822332 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6055889 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5760570 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4440053 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6010893 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6030772 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5883690 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5953937 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3408947 | OCIFISERTIB | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5766435 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5927653 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5883690 | — | k_off | = | - | s-1 | - |
| CHEMBL5982085 | — | k_off | = | - | s-1 | - |
| CHEMBL5883690 | — | kon | = | - | — | - |
| CHEMBL3408947 | OCIFISERTIB | k_off | = | - | s-1 | - |
| CHEMBL3408947 | OCIFISERTIB | kon | = | - | — | - |
| CHEMBL5814185 | — | k_off | = | - | s-1 | - |
| CHEMBL5814185 | — | kon | = | - | — | - |
| CHEMBL5814185 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL5822332 | — | k_off | = | - | s-1 | - |
| CHEMBL5927653 | — | kon | = | - | — | - |
| CHEMBL5831336 | — | k_off | = | - | s-1 | - |
| CHEMBL5831336 | — | kon | = | - | — | - |
| CHEMBL5831336 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5867004 | — | k_off | = | - | s-1 | - |
| CHEMBL5867004 | — | kon | = | - | — | - |
| CHEMBL5867004 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL6010893 | — | k_off | = | - | s-1 | - |
| CHEMBL5907354 | — | k_off | = | - | s-1 | - |
| CHEMBL4448596 | — | k_off | = | - | s-1 | - |
| CHEMBL5766613 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5873734 | — | k_off | = | - | s-1 | - |
| CHEMBL5822332 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5797099 | — | k_off | = | - | s-1 | - |
| CHEMBL5797099 | — | kon | = | - | — | - |
| CHEMBL6010893 | — | kon | = | - | — | - |
| CHEMBL5797099 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL6030782 | — | k_off | = | - | s-1 | - |
| CHEMBL5822332 | — | kon | = | - | — | - |
| CHEMBL6030782 | — | kon | = | - | — | - |
| CHEMBL6030782 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL5907354 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL5873734 | — | kon | = | - | — | - |
| CHEMBL5873734 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5953937 | — | k_off | = | - | s-1 | - |
| CHEMBL5953937 | — | kon | = | - | — | - |
| CHEMBL5760570 | — | k_off | = | - | s-1 | - |
| CHEMBL5760570 | — | kon | = | - | — | - |
| CHEMBL5927653 | — | k_off | = | - | s-1 | - |
| CHEMBL4516793 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL5907354 | — | kon | = | - | — | - |