Assay Detail
Binding
CHEMBL4401421
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Binding affinity to human FLT3 D835H mutant expressed in baculovirus expression system
7
Total Activities
7
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
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 8.50 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 9.80 |
| CHEMBL4553725 | — | — | 1 | 8.89 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.43 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.37 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.17 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.96 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105728 | CRENOLANIB | Kd | = | 0.16 | nM | 9.80 |
| CHEMBL4553725 | — | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 3.7 | nM | 8.43 |
| CHEMBL535 | SUNITINIB | Kd | = | 4.3 | nM | 8.37 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 6.8 | nM | 8.17 |
| CHEMBL1336 | SORAFENIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 14.0 | nM | 7.85 |