Assay Detail
Binding
CHEMBL4622226
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Antagonist activity at TLR9 in human PBMC assessed as inhibition of ODN2216-induced IFNalpha production preincubated for 30 mins followed by ODN2216 addition and measured after 20 hrs by alphaLISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.80 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643502 | — | — | 1 | 6.70 |
| CHEMBL4639145 | — | — | 1 | 5.70 |
| CHEMBL4646719 | — | — | 1 | 5.66 |
| CHEMBL4642538 | — | — | 1 | 5.14 |
| CHEMBL4637821 | — | — | 1 | - |
| CHEMBL4641604 | — | — | 1 | - |
| CHEMBL4641633 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643502 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4639145 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4646719 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4642538 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4637821 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641604 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641633 | — | IC50 | > | 5300.0 | nM | - |