Assay Detail
Binding
CHEMBL4815730
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Inhibition of human NOD2 expressed in HEK-blue cells coexpressing NFkappaB-SEAP reporter assessed as reduction in L18-MDP-induced NF-kappaB activation preincubated for 15 mins followed by L18-MDP stimulation and further incubated for 8 hrs by SEAP reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-Blue hNOD2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nucleotide-binding oligomerization domain-containing protein 2 (CHEMBL1293266) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.14 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4847211 | — | — | 1 | 8.52 |
| CHEMBL4853179 | — | — | 1 | 8.40 |
| CHEMBL4870434 | — | — | 1 | 8.30 |
| CHEMBL4864576 | — | — | 1 | 8.30 |
| CHEMBL4858463 | — | — | 1 | 8.05 |
| CHEMBL4859716 | — | — | 1 | 7.89 |
| CHEMBL136244 | — | — | 1 | 7.85 |
| CHEMBL136106 | — | — | 1 | 7.82 |
| CHEMBL4861488 | — | — | 1 | 7.70 |
| CHEMBL4864600 | — | — | 1 | 7.66 |
| CHEMBL49120 | PD-0166285 | 1.0 | 1 | 7.43 |
| CHEMBL4874031 | — | — | 1 | 7.03 |
| CHEMBL4868894 | — | — | 1 | 6.87 |
| CHEMBL4849134 | — | — | 1 | 6.80 |
| CHEMBL4867716 | — | — | 1 | 6.66 |
| CHEMBL4871544 | — | — | 1 | 6.57 |
| CHEMBL4875011 | — | — | 1 | 6.32 |
| CHEMBL4852513 | — | — | 1 | 6.29 |
| CHEMBL4853711 | — | — | 1 | 6.14 |
| CHEMBL4859351 | — | — | 1 | 6.06 |
| CHEMBL4852860 | — | — | 1 | 6.02 |
| CHEMBL4847571 | — | — | 1 | 5.91 |
| CHEMBL4854929 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4847211 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4853179 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4870434 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4864576 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4858463 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4859716 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL136244 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL136106 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4861488 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4864600 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL49120 | PD-0166285 | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4874031 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4868894 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4849134 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4867716 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL4871544 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4875011 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4852513 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4853711 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4859351 | — | IC50 | = | 878.0 | nM | 6.06 |
| CHEMBL4852860 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4847571 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4854929 | — | IC50 | = | 1980.0 | nM | 5.70 |