Assay Detail
Binding
CHEMBL5363601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human HPK1 catalytic domain (1 to 346 residues) using His-tagged SLP76 as substrate assessed as reduction in substrate phosphorylation preincubated for 30 mins followed by substrate and ATP addition and measured after 60 mins by TR-FRET assay
6
Total Activities
6
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 |
Target
Mitogen-activated protein kinase kinase kinase kinase 1 (CHEMBL5749) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel Diaminopyrimidine Carboxamides as HPK1 Inhibitors for Treating Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 10.56 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4859451 | — | — | 1 | 11.00 |
| CHEMBL5425184 | — | — | 1 | 10.52 |
| CHEMBL4870155 | — | — | 1 | 10.52 |
| CHEMBL5424247 | — | — | 1 | 10.52 |
| CHEMBL4848845 | — | — | 1 | 10.40 |
| CHEMBL5433529 | — | — | 1 | 10.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4859451 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5425184 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4870155 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5424247 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4848845 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL5433529 | — | IC50 | = | 0.04 | nM | 10.40 |