Assay Detail
Binding
CHEMBL4264697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human PBMC assessed as suppression of BCR-induced CD69 expression on B cells pretreated for 1 hr followed by blood stimulation measured after overnight incubation by flow cytometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.09 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4276669 | — | — | 1 | 8.85 |
| CHEMBL4279430 | — | — | 1 | 8.37 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.34 |
| CHEMBL4279353 | — | — | 1 | 8.31 |
| CHEMBL4281335 | — | — | 1 | 8.21 |
| CHEMBL4277875 | — | — | 1 | 8.15 |
| CHEMBL4285813 | — | — | 1 | 7.85 |
| CHEMBL4292583 | — | — | 1 | 7.39 |
| CHEMBL4277754 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4276669 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4279430 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4279353 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4281335 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4277875 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4285813 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4292583 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4277754 | — | IC50 | = | 44.0 | nM | 7.36 |