Assay Detail
Binding
CHEMBL5043204
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Inhibition of BTK phosphorylation in human whole blood assessed as reduction in BTK phosphorylation incubated for 30 mins
17
Total Activities
17
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 | 17 | 7.13 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080861 | — | — | 1 | 7.89 |
| CHEMBL5089327 | — | — | 1 | 7.85 |
| CHEMBL4066176 | — | — | 1 | 7.70 |
| CHEMBL5076817 | — | — | 1 | 7.68 |
| CHEMBL5083772 | BIIB-091 | 2.0 | 1 | 7.62 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 7.40 |
| CHEMBL5090290 | — | — | 1 | 7.30 |
| CHEMBL5085931 | — | — | 1 | 7.28 |
| CHEMBL5091935 | — | — | 1 | 7.22 |
| CHEMBL4209441 | SOFNOBRUTINIB | 2.0 | 1 | 7.05 |
| CHEMBL4744041 | — | — | 1 | 7.00 |
| CHEMBL3900554 | BMS-986142 | 2.0 | 1 | 6.96 |
| CHEMBL5073223 | — | — | 1 | 6.89 |
| CHEMBL5069979 | — | — | 1 | 6.82 |
| CHEMBL5087083 | — | — | 1 | 6.28 |
| CHEMBL5086077 | — | — | 1 | 6.28 |
| CHEMBL5090623 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080861 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5089327 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4066176 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5076817 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5083772 | BIIB-091 | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5090290 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5085931 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5091935 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4209441 | SOFNOBRUTINIB | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4744041 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3900554 | BMS-986142 | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5073223 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5069979 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5087083 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5086077 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5090623 | — | IC50 | = | 980.0 | nM | 6.01 |