Assay Detail
Functional
CHEMBL5502964
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Inhibition of CD69 expression on CD19+ B-cells in human whole blood pretreated for 60 mins followed by anti-IgD stimulation and measured after 18 to 22 hrs by flow cytometry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Cell Type | CD19 positive B cell |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 18 | 9.74 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5550053 | — | — | 1 | 10.59 |
| CHEMBL5557589 | — | — | 1 | 10.44 |
| CHEMBL5518143 | — | — | 1 | 10.44 |
| CHEMBL5557842 | — | — | 1 | 10.12 |
| CHEMBL5532458 | — | — | 1 | 10.10 |
| CHEMBL5527884 | — | — | 1 | 10.06 |
| CHEMBL5537092 | — | — | 1 | 9.80 |
| CHEMBL5555942 | — | — | 1 | 9.62 |
| CHEMBL5532190 | — | — | 1 | 9.59 |
| CHEMBL5555488 | — | — | 1 | 9.59 |
| CHEMBL5558638 | — | — | 1 | 9.48 |
| CHEMBL5532361 | — | — | 1 | 9.32 |
| CHEMBL5517827 | — | — | 1 | 9.13 |
| CHEMBL5549912 | — | — | 1 | 9.04 |
| CHEMBL5556300 | — | — | 1 | 8.76 |
| CHEMBL5505923 | — | — | 1 | - |
| CHEMBL5557093 | — | — | 1 | - |
| CHEMBL5512502 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5550053 | — | IC50 | = | 0.026 | nM | 10.59 |
| CHEMBL5557589 | — | IC50 | = | 0.036 | nM | 10.44 |
| CHEMBL5518143 | — | IC50 | = | 0.036 | nM | 10.44 |
| CHEMBL5557842 | — | IC50 | = | 0.075 | nM | 10.12 |
| CHEMBL5532458 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL5527884 | — | IC50 | = | 0.087 | nM | 10.06 |
| CHEMBL5537092 | — | IC50 | = | 0.157 | nM | 9.80 |
| CHEMBL5555942 | — | IC50 | = | 0.241 | nM | 9.62 |
| CHEMBL5532190 | — | IC50 | = | 0.257 | nM | 9.59 |
| CHEMBL5555488 | — | IC50 | = | 0.256 | nM | 9.59 |
| CHEMBL5558638 | — | IC50 | = | 0.333 | nM | 9.48 |
| CHEMBL5532361 | — | IC50 | = | 0.478 | nM | 9.32 |
| CHEMBL5517827 | — | IC50 | = | 0.736 | nM | 9.13 |
| CHEMBL5549912 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL5556300 | — | IC50 | = | 1.72 | nM | 8.76 |
| CHEMBL5505923 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL5557093 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL5512502 | — | IC50 | > | 10.0 | nM | - |