Assay Detail
Binding
CHEMBL4269599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RIPK2 in human whole blood assessed as reduction in MDP-stimulated TNFalpha levels incubated for 30 mins followed by MDP addition measured after 5 hrs
12
Total Activities
12
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
Receptor-interacting serine/threonine-protein kinase 2 (CHEMBL5014) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.76 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4292228 | — | — | 1 | 8.30 |
| CHEMBL4293287 | — | — | 1 | 7.96 |
| CHEMBL4289904 | — | — | 1 | 7.82 |
| CHEMBL4282034 | — | — | 1 | 7.39 |
| CHEMBL4285462 | — | — | 1 | 7.00 |
| CHEMBL4285837 | — | — | 1 | 6.81 |
| CHEMBL3823499 | — | — | 1 | 6.62 |
| CHEMBL4281602 | — | — | 1 | 6.35 |
| CHEMBL4283104 | — | — | 1 | 6.13 |
| CHEMBL4278565 | — | — | 1 | 5.86 |
| CHEMBL4293701 | — | — | 1 | 5.49 |
| CHEMBL4286477 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4292228 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4293287 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4289904 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4282034 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4285462 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4285837 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL3823499 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4281602 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL4283104 | — | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL4278565 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4293701 | — | IC50 | = | 3226.0 | nM | 5.49 |
| CHEMBL4286477 | — | IC50 | = | 4719.0 | nM | 5.33 |