Assay Detail
Binding
CHEMBL1918488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.97 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.30 |
| CHEMBL1916712 | — | — | 1 | 9.07 |
| CHEMBL1916713 | — | — | 1 | 9.07 |
| CHEMBL1916715 | — | — | 1 | 9.05 |
| CHEMBL1916888 | — | — | 1 | 8.81 |
| CHEMBL1916892 | — | — | 1 | 8.74 |
| CHEMBL1916882 | — | — | 1 | 8.72 |
| CHEMBL1916891 | — | — | 1 | 8.71 |
| CHEMBL1916714 | — | — | 1 | 8.60 |
| CHEMBL1916881 | — | — | 1 | 8.53 |
| CHEMBL1916880 | — | — | 1 | 8.48 |
| CHEMBL1916718 | — | — | 1 | 8.40 |
| CHEMBL1916897 | — | — | 1 | 8.40 |
| CHEMBL1916895 | — | — | 1 | 8.32 |
| CHEMBL1916896 | — | — | 1 | 8.30 |
| CHEMBL1916894 | — | — | 1 | 8.27 |
| CHEMBL1916899 | — | — | 1 | 8.26 |
| CHEMBL1916902 | — | — | 1 | 8.18 |
| CHEMBL1916893 | — | — | 1 | 8.17 |
| CHEMBL1916885 | — | — | 1 | 8.12 |
| CHEMBL1916901 | — | — | 1 | 8.02 |
| CHEMBL1916898 | — | — | 1 | 8.02 |
| CHEMBL1916883 | — | — | 1 | 7.99 |
| CHEMBL1916887 | — | — | 1 | 7.98 |
| CHEMBL1916889 | — | — | 1 | 7.91 |
| CHEMBL1916900 | — | — | 1 | 7.89 |
| CHEMBL1916884 | — | — | 1 | 7.88 |
| CHEMBL1916879 | — | — | 1 | 7.78 |
| CHEMBL1916717 | — | — | 1 | 7.72 |
| CHEMBL1916906 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1916712 | — | IC50 | = | 0.847 | nM | 9.07 |
| CHEMBL1916713 | — | IC50 | = | 0.847 | nM | 9.07 |
| CHEMBL1916715 | — | IC50 | = | 0.884 | nM | 9.05 |
| CHEMBL1916888 | — | IC50 | = | 1.55 | nM | 8.81 |
| CHEMBL1916892 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL1916882 | — | IC50 | = | 1.89 | nM | 8.72 |
| CHEMBL1916891 | — | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL1916714 | — | IC50 | = | 2.52 | nM | 8.60 |
| CHEMBL1916881 | — | IC50 | = | 2.96 | nM | 8.53 |
| CHEMBL1916880 | — | IC50 | = | 3.33 | nM | 8.48 |
| CHEMBL1916718 | — | IC50 | = | 3.99 | nM | 8.40 |
| CHEMBL1916897 | — | IC50 | = | 3.98 | nM | 8.40 |
| CHEMBL1916895 | — | IC50 | = | 4.83 | nM | 8.32 |
| CHEMBL1916896 | — | IC50 | = | 5.03 | nM | 8.30 |
| CHEMBL1916894 | — | IC50 | = | 5.35 | nM | 8.27 |
| CHEMBL1916899 | — | IC50 | = | 5.51 | nM | 8.26 |
| CHEMBL1916902 | — | IC50 | = | 6.58 | nM | 8.18 |
| CHEMBL1916893 | — | IC50 | = | 6.76 | nM | 8.17 |
| CHEMBL1916885 | — | IC50 | = | 7.56 | nM | 8.12 |
| CHEMBL1916898 | — | IC50 | = | 9.53 | nM | 8.02 |
| CHEMBL1916901 | — | IC50 | = | 9.53 | nM | 8.02 |
| CHEMBL1916883 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL1916887 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL1916889 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL1916900 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1916884 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL1916879 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL1916717 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL1916906 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1916716 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL1916886 | — | IC50 | = | 60.6 | nM | 7.22 |
| CHEMBL1916904 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1916890 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL1916903 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL1916907 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL1916905 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL1916719 | — | IC50 | = | 4290.0 | nM | 5.37 |