Assay Detail
Binding
CHEMBL5507154
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HPK1 (unknown origin) preincubated for 10 mins followed by ATP addition measured after 60 mins by ADP-Glo assay
53
Total Activities
53
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 novel, potent, selective and orally bioavailable HPK1 inhibitor for enhancing the efficacy of anti-PD-L1 antibody.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 7.11 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5560228 | — | — | 1 | 8.86 |
| CHEMBL5557809 | — | — | 1 | 8.74 |
| CHEMBL5558965 | — | — | 1 | 8.69 |
| CHEMBL5560445 | — | — | 1 | 8.62 |
| CHEMBL5542831 | — | — | 1 | 8.53 |
| CHEMBL5561221 | — | — | 1 | 8.53 |
| CHEMBL5556918 | — | — | 1 | 8.44 |
| CHEMBL5560869 | — | — | 1 | 8.35 |
| CHEMBL5558185 | — | — | 1 | 8.23 |
| CHEMBL5555917 | — | — | 1 | 8.14 |
| CHEMBL5555788 | — | — | 1 | 7.91 |
| CHEMBL5555659 | — | — | 1 | 7.88 |
| CHEMBL5561074 | — | — | 1 | 7.87 |
| CHEMBL5566879 | — | — | 1 | 7.78 |
| CHEMBL5557081 | — | — | 1 | 7.71 |
| CHEMBL5558967 | — | — | 1 | 7.71 |
| CHEMBL5556436 | — | — | 1 | 7.59 |
| CHEMBL5523660 | — | — | 1 | 7.55 |
| CHEMBL5557243 | — | — | 1 | 7.47 |
| CHEMBL5532543 | — | — | 1 | 7.28 |
| CHEMBL5562369 | — | — | 1 | 7.08 |
| CHEMBL5557745 | — | — | 1 | 7.02 |
| CHEMBL5549998 | — | — | 1 | 6.92 |
| CHEMBL5561800 | — | — | 1 | 6.90 |
| CHEMBL5542339 | — | — | 1 | 6.87 |
| CHEMBL5567659 | — | — | 1 | 6.85 |
| CHEMBL5560271 | — | — | 1 | 6.85 |
| CHEMBL5532107 | — | — | 1 | 6.83 |
| CHEMBL5564933 | — | — | 1 | 6.80 |
| CHEMBL5557064 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5560228 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL5557809 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5558965 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL5560445 | — | IC50 | = | 2.42 | nM | 8.62 |
| CHEMBL5542831 | — | IC50 | = | 2.96 | nM | 8.53 |
| CHEMBL5561221 | — | IC50 | = | 2.98 | nM | 8.53 |
| CHEMBL5556918 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL5560869 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5558185 | — | IC50 | = | 5.91 | nM | 8.23 |
| CHEMBL5555917 | — | IC50 | = | 7.19 | nM | 8.14 |
| CHEMBL5555788 | — | IC50 | = | 12.44 | nM | 7.91 |
| CHEMBL5555659 | — | IC50 | = | 13.29 | nM | 7.88 |
| CHEMBL5561074 | — | IC50 | = | 13.37 | nM | 7.87 |
| CHEMBL5566879 | — | IC50 | = | 16.79 | nM | 7.78 |
| CHEMBL5558967 | — | IC50 | = | 19.51 | nM | 7.71 |
| CHEMBL5557081 | — | IC50 | = | 19.49 | nM | 7.71 |
| CHEMBL5556436 | — | IC50 | = | 25.44 | nM | 7.59 |
| CHEMBL5523660 | — | IC50 | = | 28.35 | nM | 7.55 |
| CHEMBL5557243 | — | IC50 | = | 33.89 | nM | 7.47 |
| CHEMBL5532543 | — | IC50 | = | 52.28 | nM | 7.28 |
| CHEMBL5562369 | — | IC50 | = | 83.27 | nM | 7.08 |
| CHEMBL5557745 | — | IC50 | = | 95.76 | nM | 7.02 |
| CHEMBL5549998 | — | IC50 | = | 120.05 | nM | 6.92 |
| CHEMBL5561800 | — | IC50 | = | 125.1 | nM | 6.90 |
| CHEMBL5542339 | — | IC50 | = | 134.1 | nM | 6.87 |
| CHEMBL5567659 | — | IC50 | = | 142.45 | nM | 6.85 |
| CHEMBL5560271 | — | IC50 | = | 141.3 | nM | 6.85 |
| CHEMBL5532107 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5564933 | — | IC50 | = | 159.6 | nM | 6.80 |
| CHEMBL5557064 | — | IC50 | = | 161.8 | nM | 6.79 |
| CHEMBL5558031 | — | IC50 | = | 165.5 | nM | 6.78 |
| CHEMBL5559928 | — | IC50 | = | 186.55 | nM | 6.73 |
| CHEMBL5556160 | — | IC50 | = | 207.4 | nM | 6.68 |
| CHEMBL5567723 | — | IC50 | = | 227.7 | nM | 6.64 |
| CHEMBL5564823 | — | IC50 | = | 257.85 | nM | 6.59 |
| CHEMBL5532561 | — | IC50 | = | 270.1 | nM | 6.57 |
| CHEMBL5555001 | — | IC50 | = | 290.05 | nM | 6.54 |
| CHEMBL5565850 | — | IC50 | = | 291.3 | nM | 6.54 |
| CHEMBL5558624 | — | IC50 | = | 350.6 | nM | 6.46 |
| CHEMBL5518010 | — | IC50 | = | 349.45 | nM | 6.46 |
| CHEMBL5561401 | — | IC50 | = | 369.3 | nM | 6.43 |
| CHEMBL5523525 | — | IC50 | = | 446.75 | nM | 6.35 |
| CHEMBL5556179 | — | IC50 | = | 561.95 | nM | 6.25 |
| CHEMBL5532062 | — | IC50 | = | 577.95 | nM | 6.24 |
| CHEMBL5567804 | — | IC50 | = | 620.1 | nM | 6.21 |
| CHEMBL5556142 | — | IC50 | = | 648.8 | nM | 6.19 |
| CHEMBL5518077 | — | IC50 | = | 715.05 | nM | 6.15 |
| CHEMBL5566419 | — | IC50 | = | 825.45 | nM | 6.08 |
| CHEMBL5560129 | — | IC50 | = | 822.85 | nM | 6.08 |
| CHEMBL5557175 | — | IC50 | = | 910.15 | nM | 6.04 |