Assay Detail
Binding
CHEMBL4024932
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
8
Total Activities
8
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
Cytoplasmic tyrosine-protein kinase BMX (CHEMBL3834) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.82 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.10 |
| CHEMBL3290142 | — | — | 1 | 7.62 |
| CHEMBL4077064 | — | — | 1 | 7.27 |
| CHEMBL4096207 | — | — | 1 | 6.47 |
| CHEMBL4085868 | — | — | 1 | 5.87 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 5.57 |
| CHEMBL2216827 | — | — | 1 | - |
| CHEMBL4077123 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3290142 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4077064 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4096207 | — | IC50 | = | 341.3 | nM | 6.47 |
| CHEMBL4085868 | — | IC50 | = | 1359.0 | nM | 5.87 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 2665.0 | nM | 5.57 |
| CHEMBL2216827 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4077123 | — | IC50 | > | 10000.0 | nM | - |