Assay Detail
Binding
CHEMBL4053931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.28 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.47 |
| CHEMBL4071567 | — | — | 1 | 9.38 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 9.14 |
| CHEMBL4070521 | — | — | 1 | 9.04 |
| CHEMBL4092347 | — | — | 1 | 8.98 |
| CHEMBL4065460 | — | — | 1 | 8.93 |
| CHEMBL4061898 | — | — | 1 | 8.04 |
| CHEMBL4097689 | — | — | 1 | 7.62 |
| CHEMBL4094611 | — | — | 1 | 7.31 |
| CHEMBL4103300 | — | — | 1 | 7.23 |
| CHEMBL4086899 | — | — | 1 | 7.11 |
| CHEMBL4089960 | — | — | 1 | 7.07 |
| CHEMBL4074077 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4071567 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4070521 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL4092347 | — | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4065460 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL4061898 | — | IC50 | = | 9.14 | nM | 8.04 |
| CHEMBL4097689 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL4094611 | — | IC50 | = | 48.6 | nM | 7.31 |
| CHEMBL4103300 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL4086899 | — | IC50 | = | 78.6 | nM | 7.11 |
| CHEMBL4089960 | — | IC50 | = | 85.4 | nM | 7.07 |
| CHEMBL4074077 | — | IC50 | > | 100.0 | nM | - |