Assay Detail
Binding
CHEMBL3705285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time-Resolved Fluorescence Resonance Energy Transfer Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology.
12
Total Activities
9
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
Inhibitors of Bruton's tyrosine kinase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.83 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647968 | — | — | 1 | 9.28 |
| CHEMBL3647972 | — | — | 1 | 9.24 |
| CHEMBL3647973 | — | — | 2 | 9.24 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 2 | 9.14 |
| CHEMBL3647969 | — | — | 1 | 9.14 |
| CHEMBL3647964 | — | — | 1 | 8.85 |
| CHEMBL3669312 | — | — | 2 | 8.80 |
| CHEMBL3647970 | — | — | 1 | 8.60 |
| CHEMBL3647971 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647968 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL3647972 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL3647973 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL3647969 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL3647964 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3669312 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3669312 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3647970 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3647973 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3647971 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1873475 | IBRUTINIB | IC50 | < | 0.5 | nM | - |