Assay Detail
Binding
CHEMBL4689490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged HPK1 (1 to 346 residues) expressed in baculovirus infected Sf9 cells using NH2-fluorescein-RFARKGSLRQKNV-COOH as substrate incubated for 3 hrs in presence of ATP by by capillary electrophoresis method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.23 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4778959 | — | — | 1 | 9.66 |
| CHEMBL4780798 | — | — | 1 | 9.55 |
| CHEMBL4789200 | — | — | 1 | 8.92 |
| CHEMBL4750822 | — | — | 1 | 8.89 |
| CHEMBL4759406 | — | — | 1 | 8.85 |
| CHEMBL4758114 | — | — | 1 | 8.82 |
| CHEMBL4779496 | — | — | 1 | 8.66 |
| CHEMBL4748154 | — | — | 1 | 8.59 |
| CHEMBL4784181 | — | — | 1 | 8.59 |
| CHEMBL4790192 | — | — | 1 | 8.40 |
| CHEMBL4784784 | — | — | 1 | 8.40 |
| CHEMBL4761884 | — | — | 1 | 8.29 |
| CHEMBL4748045 | — | — | 1 | 8.14 |
| CHEMBL4749598 | — | — | 1 | 8.03 |
| CHEMBL4741772 | — | — | 1 | 8.00 |
| CHEMBL4745378 | — | — | 1 | 7.85 |
| CHEMBL4776227 | — | — | 1 | 7.82 |
| CHEMBL4758887 | — | — | 1 | 7.80 |
| CHEMBL4793633 | — | — | 1 | 7.70 |
| CHEMBL4758572 | — | — | 1 | 7.58 |
| CHEMBL4761304 | — | — | 1 | 7.54 |
| CHEMBL4793479 | — | — | 1 | 6.96 |
| CHEMBL4752693 | — | — | 1 | 6.14 |
| CHEMBL4792398 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4778959 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL4780798 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4789200 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4750822 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4759406 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4758114 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4779496 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4748154 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4784181 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4790192 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4784784 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4761884 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4748045 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4749598 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4741772 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4745378 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4776227 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4758887 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4793633 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4758572 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4761304 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4793479 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4752693 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4792398 | — | IC50 | > | 2000.0 | nM | - |