Assay Detail
Binding
CHEMBL5500841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HPK1 (unknown origin) using His-tagged SLP-76 as substrate preincubated for 30 mins followed by substrate and ATP addition and measured after 60 mins by TR-FRET assay
27
Total Activities
27
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
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 | 27 | 8.23 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5505932 | — | — | 1 | 9.49 |
| CHEMBL5556074 | — | — | 1 | 9.44 |
| CHEMBL5512546 | — | — | 1 | 9.37 |
| CHEMBL4878586 | — | — | 1 | 8.92 |
| CHEMBL5558035 | — | — | 1 | 8.84 |
| CHEMBL5558023 | — | — | 1 | 8.68 |
| CHEMBL5517999 | — | — | 1 | 8.61 |
| CHEMBL5556510 | — | — | 1 | 8.47 |
| CHEMBL5555827 | — | — | 1 | 8.44 |
| CHEMBL5542535 | — | — | 1 | 8.40 |
| CHEMBL5556731 | — | — | 1 | 8.39 |
| CHEMBL5556350 | — | — | 1 | 8.32 |
| CHEMBL5505883 | — | — | 1 | 8.20 |
| CHEMBL5505790 | — | — | 1 | 8.12 |
| CHEMBL5558220 | — | — | 1 | 8.07 |
| CHEMBL5559273 | — | — | 1 | 8.01 |
| CHEMBL5517850 | — | — | 1 | 7.96 |
| CHEMBL5505808 | — | — | 1 | 7.80 |
| CHEMBL5512580 | — | — | 1 | 7.77 |
| CHEMBL5527890 | — | — | 1 | 7.65 |
| CHEMBL5559247 | — | — | 1 | 7.65 |
| CHEMBL5517756 | — | — | 1 | 7.64 |
| CHEMBL5559387 | — | — | 1 | 7.36 |
| CHEMBL5537094 | — | — | 1 | 7.14 |
| CHEMBL5558221 | — | — | 1 | 7.13 |
| CHEMBL5517774 | — | — | 1 | - |
| CHEMBL5549893 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5505932 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5556074 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL5512546 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4878586 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL5558035 | — | IC50 | = | 1.45 | nM | 8.84 |
| CHEMBL5558023 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL5517999 | — | IC50 | = | 2.48 | nM | 8.61 |
| CHEMBL5556510 | — | IC50 | = | 3.39 | nM | 8.47 |
| CHEMBL5555827 | — | IC50 | = | 3.62 | nM | 8.44 |
| CHEMBL5542535 | — | IC50 | = | 3.98 | nM | 8.40 |
| CHEMBL5556731 | — | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL5556350 | — | IC50 | = | 4.79 | nM | 8.32 |
| CHEMBL5505883 | — | IC50 | = | 6.33 | nM | 8.20 |
| CHEMBL5505790 | — | IC50 | = | 7.52 | nM | 8.12 |
| CHEMBL5558220 | — | IC50 | = | 8.53 | nM | 8.07 |
| CHEMBL5559273 | — | IC50 | = | 9.81 | nM | 8.01 |
| CHEMBL5517850 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL5505808 | — | IC50 | = | 15.86 | nM | 7.80 |
| CHEMBL5512580 | — | IC50 | = | 16.93 | nM | 7.77 |
| CHEMBL5527890 | — | IC50 | = | 22.34 | nM | 7.65 |
| CHEMBL5559247 | — | IC50 | = | 22.45 | nM | 7.65 |
| CHEMBL5517756 | — | IC50 | = | 23.13 | nM | 7.64 |
| CHEMBL5559387 | — | IC50 | = | 43.44 | nM | 7.36 |
| CHEMBL5537094 | — | IC50 | = | 72.26 | nM | 7.14 |
| CHEMBL5558221 | — | IC50 | = | 74.51 | nM | 7.13 |
| CHEMBL5517774 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5549893 | — | IC50 | > | 100.0 | nM | - |