Assay Detail
Binding
CHEMBL5509529
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at N-terminal his6-tagged human recombinant NUDT5 (1 to 208 residues) expressed in Escherichia coli Rosetta (DE3) expressed in HEK293 cells incubated for 2 hrs by nanoBRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 6.83 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5557167 | — | — | 1 | 8.60 |
| CHEMBL5527860 | — | — | 1 | 5.97 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 5.91 |
| CHEMBL3707348 | ACALABRUTINIB | 4.0 | 1 | - |
| CHEMBL4297674 | BRANEBRUTINIB | 2.0 | 1 | - |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | - |
| CHEMBL4449342 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5557167 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5527860 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL1873475 | IBRUTINIB | EC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL3707348 | ACALABRUTINIB | EC50 | > | 10000.0 | nM | - |
| CHEMBL4297674 | BRANEBRUTINIB | EC50 | > | 10000.0 | nM | - |
| CHEMBL4072833 | EVOBRUTINIB | EC50 | > | 10000.0 | nM | - |
| CHEMBL4449342 | — | EC50 | > | 10000.0 | nM | - |