Assay Detail
Binding
CHEMBL4385972
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Inhibition of recombinant human FLT3 (564 to end residues) using EAIYAAPFAKKK as substrate measured after 40 mins in presence of [gamma-33P]-ATP by scintillation counting analysis
40
Total Activities
40
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
Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.66 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4551114 | — | — | 1 | 8.40 |
| CHEMBL4517711 | — | — | 1 | 8.22 |
| CHEMBL4435457 | — | — | 1 | 8.22 |
| CHEMBL4439404 | — | — | 1 | 8.15 |
| CHEMBL4572972 | — | — | 1 | 8.15 |
| CHEMBL4557634 | — | — | 1 | 8.15 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.13 |
| CHEMBL4572804 | — | — | 1 | 8.05 |
| CHEMBL4440175 | — | — | 1 | 8.05 |
| CHEMBL4441629 | — | — | 1 | 8.05 |
| CHEMBL4459941 | — | — | 1 | 7.89 |
| CHEMBL4441875 | — | — | 1 | 7.82 |
| CHEMBL4541344 | — | — | 1 | 7.80 |
| CHEMBL4475375 | — | — | 1 | 7.77 |
| CHEMBL4454804 | — | — | 1 | 7.77 |
| CHEMBL4461531 | — | — | 1 | 7.72 |
| CHEMBL4435360 | — | — | 1 | 7.70 |
| CHEMBL4515336 | — | — | 1 | 7.70 |
| CHEMBL4575519 | — | — | 1 | 7.68 |
| CHEMBL4472511 | — | — | 1 | 7.66 |
| CHEMBL4526888 | — | — | 1 | 7.60 |
| CHEMBL4539069 | — | — | 1 | 7.58 |
| CHEMBL4438587 | — | — | 1 | 7.58 |
| CHEMBL4569015 | — | — | 1 | 7.52 |
| CHEMBL4586009 | — | — | 1 | 7.51 |
| CHEMBL4529106 | — | — | 1 | 7.50 |
| CHEMBL4532475 | — | — | 1 | 7.50 |
| CHEMBL4449006 | — | — | 1 | 7.47 |
| CHEMBL4553847 | — | — | 1 | 7.43 |
| CHEMBL4591906 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4551114 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4517711 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4435457 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4439404 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4572972 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4557634 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4572804 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4440175 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4441629 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4459941 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4441875 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4541344 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4475375 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4454804 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4461531 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4435360 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4515336 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4575519 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4472511 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4526888 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4438587 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4539069 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4569015 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4586009 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4529106 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4532475 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4449006 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4553847 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4591906 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4483045 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4439044 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4558160 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4553033 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4442278 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4457542 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4551816 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4533761 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4468986 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4449318 | — | IC50 | - | — | - |