Assay Detail
Binding
CHEMBL4178245
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C57BL/6J mouse BTK assessed as decrease in anti-mouse IgM antibody stimulated BCR mediated CD69 upregulation preincubated for 30 mins followed by antibody challenge after 18 to 24 hrs by flow cytometry
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.59 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3928203 | — | — | 1 | 8.26 |
| CHEMBL3936823 | — | — | 1 | 8.24 |
| CHEMBL3967108 | — | — | 1 | 8.08 |
| CHEMBL3959033 | — | — | 1 | 8.08 |
| CHEMBL3922230 | — | — | 1 | 7.85 |
| CHEMBL3982806 | — | — | 1 | 7.83 |
| CHEMBL3891434 | — | — | 1 | 7.75 |
| CHEMBL3891185 | — | — | 1 | 7.50 |
| CHEMBL3968892 | — | — | 1 | 7.44 |
| CHEMBL3966346 | — | — | 1 | 7.38 |
| CHEMBL3921350 | — | — | 1 | 7.32 |
| CHEMBL4216939 | — | — | 1 | 7.29 |
| CHEMBL3900184 | — | — | 1 | 7.29 |
| CHEMBL3962146 | — | — | 1 | 7.27 |
| CHEMBL3935716 | — | — | 1 | 7.23 |
| CHEMBL3946460 | — | — | 1 | 7.12 |
| CHEMBL3907763 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3928203 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3936823 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3967108 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3959033 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3922230 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3982806 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL3891434 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL3891185 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3968892 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3966346 | — | IC50 | = | 41.9 | nM | 7.38 |
| CHEMBL3921350 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4216939 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL3900184 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3962146 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3935716 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3946460 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3907763 | — | IC50 | = | 81.0 | nM | 7.09 |