Assay Detail
Binding
CHEMBL5584589
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RIPK2 in MDP stimulated NOD2 in human THP-1 cells expressing luciaTM NF-kappaB assessed as reduction in NF-Kappa B activation measured after 24 hrs by QUANTI-Luc reagent based luminescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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
Design, synthesis and evaluation of novel thieno[2,3d]pyrimidine derivatives as potent and specific RIPK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.55 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514780 | — | — | 1 | 7.42 |
| CHEMBL5596475 | — | — | 1 | 7.30 |
| CHEMBL5597467 | — | — | 1 | 6.95 |
| CHEMBL5597795 | — | — | 1 | 6.89 |
| CHEMBL5596824 | — | — | 1 | 6.85 |
| CHEMBL5598306 | — | — | 1 | 6.81 |
| CHEMBL5596566 | — | — | 1 | 6.78 |
| CHEMBL5597463 | — | — | 1 | 6.71 |
| CHEMBL5596171 | — | — | 1 | 6.67 |
| CHEMBL5596719 | — | — | 1 | 6.64 |
| CHEMBL5597383 | — | — | 1 | 6.48 |
| CHEMBL5597382 | — | — | 1 | 6.32 |
| CHEMBL5590947 | — | — | 1 | 6.25 |
| CHEMBL5596401 | — | — | 1 | 5.92 |
| CHEMBL5597496 | — | — | 1 | 5.53 |
| CHEMBL5598319 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514780 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5596475 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5597467 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL5597795 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5596824 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5598306 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5596566 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5597463 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL5596171 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5596719 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5597383 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL5597382 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL5590947 | — | IC50 | = | 569.0 | nM | 6.25 |
| CHEMBL5596401 | — | IC50 | = | 1203.0 | nM | 5.92 |
| CHEMBL5597496 | — | IC50 | = | 2976.0 | nM | 5.53 |
| CHEMBL5598319 | — | IC50 | = | 5029.0 | nM | 5.30 |