Assay Detail
Binding
CHEMBL5328398
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human HPK1 in human Jurkat cells assessed as reduction in SLP76 phosphorylation at Ser376 residue preincubated for 60 mins followed by alphaCD3/alphaCD28 DynabeadsTM stimulation for 15 mins by AlphaLISA assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| 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 quinazoline HPK1 inhibitors with high cellular potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.46 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5408958 | — | — | 1 | 10.01 |
| CHEMBL5407240 | — | — | 1 | 9.05 |
| CHEMBL5403001 | — | — | 1 | 8.80 |
| CHEMBL5421924 | — | — | 1 | 8.70 |
| CHEMBL5401820 | — | — | 1 | 8.52 |
| CHEMBL5405626 | — | — | 1 | 8.52 |
| CHEMBL5396156 | — | — | 1 | 8.52 |
| CHEMBL5427316 | — | — | 1 | 8.30 |
| CHEMBL5400089 | — | — | 1 | 8.30 |
| CHEMBL5420868 | — | — | 1 | 8.05 |
| CHEMBL5439907 | — | — | 1 | 8.00 |
| CHEMBL5418553 | — | — | 1 | 7.96 |
| CHEMBL5394698 | — | — | 1 | 7.96 |
| CHEMBL5420966 | — | — | 1 | 7.85 |
| CHEMBL5428695 | — | — | 1 | 7.82 |
| CHEMBL5417747 | — | — | 1 | 7.77 |
| CHEMBL5407935 | — | — | 1 | 7.64 |
| CHEMBL5406408 | — | — | 1 | 7.64 |
| CHEMBL5409078 | — | — | 1 | 7.52 |
| CHEMBL5420652 | — | — | 1 | 7.52 |
| CHEMBL5395026 | — | — | 1 | 7.42 |
| CHEMBL5401088 | — | — | 1 | 7.28 |
| CHEMBL5420011 | — | — | 1 | 7.23 |
| CHEMBL5425004 | — | — | 1 | 7.22 |
| CHEMBL5439204 | — | — | 1 | 7.14 |
| CHEMBL5423968 | — | — | 1 | 7.08 |
| CHEMBL5407643 | — | — | 1 | 7.00 |
| CHEMBL5424400 | — | — | 1 | 6.92 |
| CHEMBL5396693 | — | — | 1 | 6.89 |
| CHEMBL5411794 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408958 | — | IC50 | = | 0.097 | nM | 10.01 |
| CHEMBL5407240 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL5403001 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5421924 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5401820 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5405626 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5396156 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5427316 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5400089 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5420868 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5439907 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5418553 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5394698 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5420966 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5428695 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5417747 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5407935 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5406408 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5409078 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5420652 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5395026 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5401088 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5420011 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5425004 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5439204 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5423968 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5407643 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5424400 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5396693 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5411794 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5421672 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5395638 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5441105 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5412652 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5430021 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5440958 | — | IC50 | = | 809.0 | nM | 6.09 |
| CHEMBL5400101 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5394328 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5420572 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5428061 | — | IC50 | > | 10000.0 | nM | - |