Assay Detail
Binding
CHEMBL5502958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK (unknown origin) using fluorescein labeled polyGAT peptide substrate incubated for 30 mins in presence of ATP by time-resolved fluorescence assay
4
Total Activities
4
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 and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.33 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5558638 | — | — | 1 | 9.30 |
| CHEMBL5549935 | — | — | 1 | 8.47 |
| CHEMBL5505806 | — | — | 1 | 8.34 |
| CHEMBL5555158 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5558638 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5549935 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5505806 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5555158 | — | IC50 | = | 63.0 | nM | 7.20 |