Assay Detail
Binding
CHEMBL5225524
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human wild type FLT3 using TK peptide as substrate incubated for 1 hr in presence of ATP by HTRF assay
25
Total Activities
25
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
Design, synthesis, and evaluation of pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as potent FLT3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.51 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.70 |
| CHEMBL5288494 | — | — | 1 | 7.30 |
| CHEMBL5271605 | — | — | 1 | 7.21 |
| CHEMBL5282636 | — | — | 1 | 7.14 |
| CHEMBL5287072 | — | — | 1 | 7.07 |
| CHEMBL5273130 | — | — | 1 | 6.99 |
| CHEMBL5276264 | — | — | 1 | 6.99 |
| CHEMBL5268304 | — | — | 1 | 6.99 |
| CHEMBL5265945 | — | — | 1 | 6.91 |
| CHEMBL5273214 | — | — | 1 | 6.78 |
| CHEMBL5289344 | — | — | 1 | 6.73 |
| CHEMBL5273845 | — | — | 1 | 6.71 |
| CHEMBL5285412 | — | — | 1 | 6.54 |
| CHEMBL5270170 | — | — | 1 | 6.36 |
| CHEMBL5288830 | — | — | 1 | 6.22 |
| CHEMBL5279939 | — | — | 1 | 6.13 |
| CHEMBL5282407 | — | — | 1 | 6.07 |
| CHEMBL5280904 | — | — | 1 | 6.04 |
| CHEMBL5291209 | — | — | 1 | 6.03 |
| CHEMBL5271010 | — | — | 1 | 5.98 |
| CHEMBL5286747 | — | — | 1 | 5.66 |
| CHEMBL5285568 | — | — | 1 | 5.60 |
| CHEMBL5288327 | — | — | 1 | 5.57 |
| CHEMBL5266530 | — | — | 1 | 5.42 |
| CHEMBL5278770 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5288494 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5271605 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5282636 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5287072 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5273130 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5276264 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5268304 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5265945 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5273214 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5289344 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL5273845 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5285412 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL5270170 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5288830 | — | IC50 | = | 599.0 | nM | 6.22 |
| CHEMBL5279939 | — | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL5282407 | — | IC50 | = | 856.0 | nM | 6.07 |
| CHEMBL5280904 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL5291209 | — | IC50 | = | 939.0 | nM | 6.03 |
| CHEMBL5271010 | — | IC50 | = | 1042.0 | nM | 5.98 |
| CHEMBL5286747 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL5285568 | — | IC50 | = | 2537.0 | nM | 5.60 |
| CHEMBL5288327 | — | IC50 | = | 2722.0 | nM | 5.57 |
| CHEMBL5266530 | — | IC50 | = | 3826.0 | nM | 5.42 |
| CHEMBL5278770 | — | IC50 | > | 10.0 | nM | - |