Assay Detail
Binding
CHEMBL2183762
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLT3 D835Y mutant expressed in human MV4-11 cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 8.22 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | IC50 | = | 6.0 | nM | 8.22 |