Assay Detail
Binding
CHEMBL5628446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal polyHis-tagged human RIPK2 (8 to 310 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
36
Total Activities
36
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 2 (CHEMBL5014) ↗| 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 | 36 | 7.96 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779280 | — | — | 1 | 8.70 |
| CHEMBL5631858 | — | — | 1 | 8.52 |
| CHEMBL5631966 | — | — | 1 | 8.52 |
| CHEMBL5632745 | — | — | 1 | 8.40 |
| CHEMBL5632664 | — | — | 1 | 8.40 |
| CHEMBL5631969 | — | — | 1 | 8.40 |
| CHEMBL5632081 | — | — | 1 | 8.40 |
| CHEMBL5632677 | — | — | 1 | 8.40 |
| CHEMBL5632272 | — | — | 1 | 8.40 |
| CHEMBL4596287 | — | — | 1 | 8.40 |
| CHEMBL5632508 | — | — | 1 | 8.30 |
| CHEMBL5633841 | — | — | 1 | 8.30 |
| CHEMBL5632238 | — | — | 1 | 8.30 |
| CHEMBL5631246 | — | — | 1 | 8.30 |
| CHEMBL5632098 | — | — | 1 | 8.30 |
| CHEMBL5633433 | — | — | 1 | 8.22 |
| CHEMBL5633099 | — | — | 1 | 8.22 |
| CHEMBL5633512 | — | — | 1 | 8.15 |
| CHEMBL5631880 | — | — | 1 | 8.10 |
| CHEMBL5632130 | — | — | 1 | 8.05 |
| CHEMBL5633137 | — | — | 1 | 8.00 |
| CHEMBL5631523 | — | — | 1 | 8.00 |
| CHEMBL5632875 | — | — | 1 | 8.00 |
| CHEMBL5632398 | — | — | 1 | 7.96 |
| CHEMBL5632423 | — | — | 1 | 7.92 |
| CHEMBL5631683 | — | — | 1 | 7.85 |
| CHEMBL5632899 | — | — | 1 | 7.85 |
| CHEMBL5633010 | — | — | 1 | 7.75 |
| CHEMBL5633859 | — | — | 1 | 7.75 |
| CHEMBL5632922 | — | — | 1 | 7.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779280 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5631858 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5631966 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5632745 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632664 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5631969 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632081 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632677 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632272 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4596287 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632508 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5632098 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5631246 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5632238 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5633841 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5633433 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5633099 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5633512 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5631880 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5632130 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5633137 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5631523 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5632875 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5632398 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5632423 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5631683 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5632899 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5633010 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5633859 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5632922 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5632322 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5632306 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5633313 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5633797 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5631295 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL5631682 | — | IC50 | = | 3900.0 | nM | 5.41 |