Assay Detail
Binding
CHEMBL5043205
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CD69 in human whole blood preincubated for 30 mins followed by anti-human IgD stimulation and measured after 18 to 22 hrs by flow cytometry
27
Total Activities
27
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
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.49 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080861 | — | — | 1 | 8.00 |
| CHEMBL4066176 | — | — | 1 | 7.40 |
| CHEMBL5088454 | — | — | 1 | 7.40 |
| CHEMBL5076817 | — | — | 1 | 7.23 |
| CHEMBL5083772 | BIIB-091 | 2.0 | 1 | 7.16 |
| CHEMBL5085192 | — | — | 1 | 7.00 |
| CHEMBL5085931 | — | — | 1 | 6.98 |
| CHEMBL5083323 | — | — | 1 | 6.89 |
| CHEMBL5094998 | — | — | 1 | 6.70 |
| CHEMBL4650323 | TOLEBRUTINIB | 3.0 | 1 | 6.70 |
| CHEMBL5084997 | — | — | 1 | 6.66 |
| CHEMBL5089327 | — | — | 1 | 6.48 |
| CHEMBL5090589 | — | — | 1 | 6.41 |
| CHEMBL5081318 | — | — | 1 | 6.40 |
| CHEMBL5090290 | — | — | 1 | 6.40 |
| CHEMBL5073995 | — | — | 1 | 6.16 |
| CHEMBL5093189 | — | — | 1 | 6.10 |
| CHEMBL5087011 | — | — | 1 | 6.07 |
| CHEMBL4163691 | POSELTINIB | 2.0 | 1 | 6.01 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 5.96 |
| CHEMBL4209441 | SOFNOBRUTINIB | 2.0 | 1 | 5.92 |
| CHEMBL5069979 | — | — | 1 | 5.92 |
| CHEMBL3900554 | BMS-986142 | 2.0 | 1 | 5.89 |
| CHEMBL5075191 | — | — | 1 | 5.80 |
| CHEMBL4744041 | — | — | 1 | 5.52 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 5.51 |
| CHEMBL5083788 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080861 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4066176 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5088454 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5076817 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5083772 | BIIB-091 | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5085192 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5085931 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5083323 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5094998 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4650323 | TOLEBRUTINIB | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5084997 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5089327 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5090589 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5081318 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5090290 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5073995 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5093189 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5087011 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4163691 | POSELTINIB | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4209441 | SOFNOBRUTINIB | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5069979 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3900554 | BMS-986142 | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5075191 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4744041 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5083788 | — | IC50 | > | 10000.0 | nM | - |