Assay Detail
Binding
CHEMBL4701067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal His6-tagged BTK expressed in baculovirus infected Sf21 insect cells using fluorescein-labeled polyGAT peptide substrate measured after 30 mins by TR-FRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.16 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4782313 | — | — | 1 | 9.70 |
| CHEMBL4754065 | — | — | 1 | 9.70 |
| CHEMBL4796367 | — | — | 1 | 9.40 |
| CHEMBL4746275 | — | — | 1 | 9.40 |
| CHEMBL4744041 | — | — | 1 | 9.00 |
| CHEMBL4797536 | — | — | 1 | 8.77 |
| CHEMBL4788285 | — | — | 1 | 8.74 |
| CHEMBL4760128 | — | — | 1 | 8.70 |
| CHEMBL4749757 | — | — | 1 | 8.70 |
| CHEMBL4792826 | — | — | 1 | 8.68 |
| CHEMBL4740150 | — | — | 1 | 8.52 |
| CHEMBL4756023 | — | — | 1 | 8.30 |
| CHEMBL4783488 | — | — | 1 | 8.22 |
| CHEMBL4764045 | — | — | 1 | 8.05 |
| CHEMBL4753530 | — | — | 1 | 8.00 |
| CHEMBL4763987 | — | — | 1 | 7.82 |
| CHEMBL4791140 | — | — | 1 | 7.50 |
| CHEMBL4741954 | — | — | 1 | 7.40 |
| CHEMBL4778259 | — | — | 1 | 7.03 |
| CHEMBL4755663 | — | — | 1 | 6.85 |
| CHEMBL4757354 | — | — | 1 | 5.50 |
| CHEMBL4789778 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4782313 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4754065 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4796367 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4746275 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4744041 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4797536 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4788285 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4760128 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4749757 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4792826 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4740150 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4756023 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4783488 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4764045 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4753530 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4763987 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4791140 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4741954 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4778259 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4755663 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4757354 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4789778 | — | IC50 | = | 3700.0 | nM | 5.43 |