Assay Detail
Binding
CHEMBL4668242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human whole blood assessed as reduction in polyclonal anti-IgM antibody/human IL4-stimulated CD69 cell surface expression on B cells incubated for 16 hrs by FACS analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.69 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4795673 | — | — | 1 | 7.80 |
| CHEMBL4739958 | — | — | 1 | 7.72 |
| CHEMBL4749522 | — | — | 1 | 7.58 |
| CHEMBL4593663 | — | — | 1 | 7.50 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.18 |
| CHEMBL4789435 | — | — | 1 | 7.18 |
| CHEMBL4740933 | — | — | 1 | 6.65 |
| CHEMBL4746262 | — | — | 1 | 6.52 |
| CHEMBL4762397 | — | — | 1 | 6.03 |
| CHEMBL4793026 | — | — | 1 | 5.90 |
| CHEMBL4788086 | — | — | 1 | 5.13 |
| CHEMBL4744271 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4795673 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4739958 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4749522 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4593663 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4789435 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4740933 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL4746262 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL4762397 | — | IC50 | = | 934.0 | nM | 6.03 |
| CHEMBL4793026 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4788086 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL4744271 | — | IC50 | = | 8000.0 | nM | 5.10 |