Assay Detail
Binding
CHEMBL4726196
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged TXK (260 to 527 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
5
Total Activities
5
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 |
Publication
Discovery of quinoline-based irreversible BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.20 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.70 |
| CHEMBL4755977 | — | — | 1 | 7.72 |
| CHEMBL4782725 | — | — | 1 | 6.64 |
| CHEMBL4752700 | — | — | 1 | 6.53 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4755977 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4782725 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL4752700 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 368.0 | nM | 6.43 |