Assay Detail
Binding
CHEMBL4252316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.52 |
| CHEMBL4294772 | — | — | 1 | 9.30 |
| CHEMBL4290692 | — | — | 1 | 9.22 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 9.22 |
| CHEMBL4284156 | — | — | 1 | 9.15 |
| CHEMBL4290449 | — | — | 1 | 9.15 |
| CHEMBL4286900 | — | — | 1 | 9.10 |
| CHEMBL4289281 | — | — | 1 | 9.10 |
| CHEMBL4289688 | — | — | 1 | 9.00 |
| CHEMBL4278652 | — | — | 1 | 7.98 |
| CHEMBL4280709 | — | — | 1 | 7.77 |
| CHEMBL4292468 | — | — | 1 | 7.50 |
| CHEMBL4287960 | — | — | 1 | 7.09 |
| CHEMBL4277319 | — | — | 1 | 7.05 |
| CHEMBL4279066 | — | — | 1 | 7.05 |
| CHEMBL4284578 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4294772 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4290692 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4284156 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4290449 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4286900 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4289281 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4289688 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4278652 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL4280709 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL4292468 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL4287960 | — | IC50 | = | 81.7 | nM | 7.09 |
| CHEMBL4277319 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4279066 | — | IC50 | = | 89.32 | nM | 7.05 |
| CHEMBL4284578 | — | IC50 | > | 100.0 | nM | - |