Assay Detail
Binding
CHEMBL5628447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal polyHis-tagged human RIPK3 (1 to 307 residues) expressed in Sf9 cells using MBP as substrate preincubated for 15 mins followed by ATP addition measured after 90 mins by ADP-Glo assay
17
Total Activities
17
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
Receptor-interacting serine/threonine-protein kinase 3 (CHEMBL1795199) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploring positions 6 and 7 of a quinazoline-based scaffold leads to changes in selectivity and potency towards RIPK2/3 kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.14 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779280 | — | — | 1 | 7.11 |
| CHEMBL5631858 | — | — | 1 | 6.93 |
| CHEMBL5632745 | — | — | 1 | 6.91 |
| CHEMBL5632238 | — | — | 1 | 6.85 |
| CHEMBL5632098 | — | — | 1 | 6.42 |
| CHEMBL5633099 | — | — | 1 | 6.41 |
| CHEMBL5632272 | — | — | 1 | 6.40 |
| CHEMBL5633841 | — | — | 1 | 6.33 |
| CHEMBL5631246 | — | — | 1 | 6.26 |
| CHEMBL5632081 | — | — | 1 | 5.82 |
| CHEMBL5633859 | — | — | 1 | 5.80 |
| CHEMBL5632322 | — | — | 1 | 5.72 |
| CHEMBL5633433 | — | — | 1 | 5.68 |
| CHEMBL5631295 | — | — | 1 | 5.58 |
| CHEMBL5632922 | — | — | 1 | 5.54 |
| CHEMBL5633010 | — | — | 1 | 5.44 |
| CHEMBL5632677 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779280 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5631858 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5632745 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5632238 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5632098 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL5633099 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL5632272 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL5633841 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL5631246 | — | IC50 | = | 551.0 | nM | 6.26 |
| CHEMBL5632081 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5633859 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5632322 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5633433 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5631295 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5632922 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5633010 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5632677 | — | IC50 | = | 6000.0 | nM | 5.22 |