Assay Detail
Binding
CHEMBL5500842
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal nanoluc-fused HPK1 (unknown origin) expressed in HEK293T cells preincubated for 2 hrs in presence of cell permeable fluorescent probe 5 followed by substrate addition and measured after 5 mins by Nano-BRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase kinase 1 (CHEMBL5749) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 5-aminopyrido[2,3-d]pyrimidin-7(8H)-one derivatives as new hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.75 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5505932 | — | — | 1 | 7.30 |
| CHEMBL5512546 | — | — | 1 | 7.22 |
| CHEMBL5556074 | — | — | 1 | 6.54 |
| CHEMBL4878586 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5505932 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5512546 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5556074 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4878586 | — | IC50 | = | 1120.0 | nM | 5.95 |