Assay Detail
Binding
CHEMBL4610787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay
23
Total Activities
23
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 boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.17 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.52 |
| CHEMBL4642642 | — | — | 1 | 9.22 |
| CHEMBL4640647 | — | — | 1 | 8.82 |
| CHEMBL4649397 | — | — | 1 | 8.77 |
| CHEMBL4648104 | — | — | 1 | 8.72 |
| CHEMBL4645290 | — | — | 1 | 8.70 |
| CHEMBL4648837 | — | — | 1 | 8.54 |
| CHEMBL4647555 | — | — | 1 | 8.33 |
| CHEMBL4647822 | — | — | 1 | 8.21 |
| CHEMBL4640192 | — | — | 1 | 8.19 |
| CHEMBL4647100 | — | — | 1 | 8.19 |
| CHEMBL4648257 | — | — | 1 | 8.09 |
| CHEMBL4647623 | — | — | 1 | 8.07 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 8.01 |
| CHEMBL4640054 | — | — | 1 | 7.93 |
| CHEMBL4633949 | — | — | 1 | 7.43 |
| CHEMBL4635803 | — | — | 1 | 7.20 |
| CHEMBL4639063 | — | — | 1 | 6.81 |
| CHEMBL4639665 | — | — | 1 | 6.57 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | - |
| CHEMBL4647525 | — | — | 1 | - |
| CHEMBL4649339 | — | — | 1 | - |
| CHEMBL4637760 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4642642 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4640647 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4649397 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4648104 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4645290 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4648837 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4647555 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4647822 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4640192 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4647100 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4648257 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4647623 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4640054 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL4633949 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL4635803 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4639063 | — | IC50 | = | 156.2 | nM | 6.81 |
| CHEMBL4639665 | — | IC50 | = | 267.8 | nM | 6.57 |
| CHEMBL221959 | TOFACITINIB | IC50 | > | 100.0 | nM | - |
| CHEMBL4647525 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4649339 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4637760 | — | IC50 | > | 1000.0 | nM | - |