Assay Detail
Binding
CHEMBL5584588
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RIPK2 in C14-Tri-LAN-Gly stimulated NOD1 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
13
Total Activities
13
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 | 13 | 6.58 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514780 | — | — | 1 | 7.04 |
| CHEMBL5596475 | — | — | 1 | 6.96 |
| CHEMBL5596824 | — | — | 1 | 6.78 |
| CHEMBL5597795 | — | — | 1 | 6.76 |
| CHEMBL5597463 | — | — | 1 | 6.74 |
| CHEMBL5598474 | — | — | 1 | 6.61 |
| CHEMBL5596566 | — | — | 1 | 6.59 |
| CHEMBL5597382 | — | — | 1 | 6.49 |
| CHEMBL5596719 | — | — | 1 | 6.44 |
| CHEMBL5596171 | — | — | 1 | 6.39 |
| CHEMBL5597383 | — | — | 1 | 6.36 |
| CHEMBL5597467 | — | — | 1 | 6.29 |
| CHEMBL5590947 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514780 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5596475 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5596824 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5597795 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5597463 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL5598474 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL5596566 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL5597382 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5596719 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL5596171 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL5597383 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL5597467 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL5590947 | — | IC50 | = | 734.0 | nM | 6.13 |