Assay Detail
Binding
CHEMBL5135990
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Antagonist activity at gardiquimod stimulated human TRL7 overexpressed in HEK293 cells assessed as inhibition of NF kappa B/Ap-1 activation preincubated with compound for 30 mins followed by gardiquimod stimulation measured after 22 hrs by SEAP reporter assay
34
Total Activities
34
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 | 34 | 7.40 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5201891 | — | — | 1 | 9.15 |
| CHEMBL5182126 | — | — | 1 | 9.10 |
| CHEMBL5176097 | — | — | 1 | 9.05 |
| CHEMBL5169693 | — | — | 1 | 8.74 |
| CHEMBL5201981 | — | — | 1 | 8.72 |
| CHEMBL5178588 | — | — | 1 | 8.59 |
| CHEMBL5190495 | — | — | 1 | 8.21 |
| CHEMBL5183412 | — | — | 1 | 8.14 |
| CHEMBL5201441 | — | — | 1 | 8.09 |
| CHEMBL5174201 | — | — | 1 | 7.89 |
| CHEMBL5180395 | — | — | 1 | 7.85 |
| CHEMBL5176324 | — | — | 1 | 7.77 |
| CHEMBL5197134 | — | — | 1 | 7.66 |
| CHEMBL5179092 | — | — | 1 | 7.62 |
| CHEMBL5179188 | — | — | 1 | 7.55 |
| CHEMBL5184042 | — | — | 1 | 7.55 |
| CHEMBL5188600 | — | — | 1 | 7.54 |
| CHEMBL5186413 | — | — | 1 | 7.24 |
| CHEMBL5194452 | — | — | 1 | 7.13 |
| CHEMBL5196314 | — | — | 1 | 7.09 |
| CHEMBL5175964 | — | — | 1 | 7.04 |
| CHEMBL5179724 | — | — | 1 | 7.01 |
| CHEMBL5204983 | — | — | 1 | 6.70 |
| CHEMBL4647818 | — | — | 1 | 6.60 |
| CHEMBL5205027 | — | — | 1 | 6.52 |
| CHEMBL5173429 | — | — | 1 | 6.28 |
| CHEMBL5189004 | — | — | 1 | 6.26 |
| CHEMBL5191852 | — | — | 1 | 6.21 |
| CHEMBL5192984 | — | — | 1 | 5.48 |
| CHEMBL4645620 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5201891 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5182126 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5176097 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5169693 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5201981 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5178588 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5190495 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5183412 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5201441 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5174201 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5180395 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5176324 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5197134 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5179092 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5184042 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5179188 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5188600 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5186413 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5194452 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5196314 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5175964 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5179724 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5204983 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4647818 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5205027 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5173429 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5189004 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5191852 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5192984 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4645620 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4636988 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5189738 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5197502 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5209157 | — | IC50 | > | 10000.0 | nM | - |