Assay Detail
Binding
CHEMBL5135992
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Antagonist activity at ODN2006 stimulated human TRL9 overexpressed in HEK293 cells assessed as inhibition of NF kappa B/Ap-1 activation preincubated with compound for 30 mins followed by ODN2006 stimulation measured after 22 hrs by SEAP reporter assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of 2-Pyridinylindole-Based Dual Antagonists of Toll-like Receptors 7 and 8 (TLR7/8).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.01 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5201891 | — | — | 1 | 6.46 |
| CHEMBL4647818 | — | — | 1 | 6.37 |
| CHEMBL4645620 | — | — | 1 | 6.30 |
| CHEMBL5189004 | — | — | 1 | 6.24 |
| CHEMBL5192984 | — | — | 1 | 6.20 |
| CHEMBL5209157 | — | — | 1 | 6.09 |
| CHEMBL5173429 | — | — | 1 | 5.82 |
| CHEMBL4636988 | — | — | 1 | 5.72 |
| CHEMBL5189738 | — | — | 1 | 5.55 |
| CHEMBL5197502 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5201891 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4647818 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4645620 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5189004 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5192984 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5209157 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5173429 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4636988 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5189738 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5197502 | — | IC50 | = | 4600.0 | nM | 5.34 |