Assay Detail
Binding
CHEMBL3864052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay
15
Total Activities
15
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
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a N,9-Diphenyl-9H-purin-2-amine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.52 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.52 |
| CHEMBL3893465 | — | — | 1 | 9.40 |
| CHEMBL3953720 | — | — | 1 | 9.30 |
| CHEMBL3966494 | — | — | 1 | 9.30 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 9.22 |
| CHEMBL3975003 | — | — | 1 | 7.99 |
| CHEMBL3982421 | — | — | 1 | 7.88 |
| CHEMBL3975962 | — | — | 1 | 7.82 |
| CHEMBL3919900 | — | — | 1 | 7.77 |
| CHEMBL3962478 | — | — | 1 | 7.01 |
| CHEMBL3973451 | — | — | 1 | - |
| CHEMBL3963986 | — | — | 1 | - |
| CHEMBL3946985 | — | — | 1 | - |
| CHEMBL3895185 | — | — | 1 | - |
| CHEMBL3904111 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3893465 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3953720 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3966494 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3975003 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL3982421 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3975962 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL3919900 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3962478 | — | IC50 | = | 97.1 | nM | 7.01 |
| CHEMBL3973451 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL3963986 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL3946985 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL3895185 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL3904111 | — | IC50 | > | 100.0 | nM | - |