Assay Detail
Binding
CHEMBL5734691
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Interleukin 6 Induction Assay: Compounds diluted in DMSO were transferred to individual wells of a Matrix Technologies clear, V-bottom 384-well plate using ECHO acoustic liquid handling technology (25 nL per well). Human whole-blood samples (25 uL) were added to each well using a CyBio FeliX liquid handling instrument. The plate was shaken on a plate shaker for three min before incubating the reaction mixtures at 37° C. for 20 h. Basel RPMI 1640 medium (supplemented with L-glutamine) was then added to each well (25 uL per well) prior to liberating plasma from each sample by centrifugation (450×g, 5 min, ambient temperature). Treated plasma samples (3 uL) were subsequently transferred to individual wells of a white, shallow, 384-well ProxiPlate (Perkin Elmer) using the FeliX liquid handling instrument and their interleukin 6 levels were measured using AlphaLISA technology as described by the manufacturer, PerkinElmer. Data analyses software was used to determine compound EC50 values where the baseline was established using average DMSO values and 100% induction established using reference compound values at the highest concentration tested. EC50's can be determined with software such as Graphpad Prism.
171
Total Activities
54
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 57 | 7.60 | 8.60 |
| kon | 57 | - | - |
| k_off | 57 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5967615 | — | — | 3 | 8.60 |
| CHEMBL5757665 | — | — | 3 | 8.42 |
| CHEMBL5993886 | — | — | 3 | 8.42 |
| CHEMBL5977638 | — | — | 6 | 8.29 |
| CHEMBL5790478 | — | — | 3 | 8.24 |
| CHEMBL5992328 | — | — | 3 | 8.23 |
| CHEMBL6041191 | — | — | 3 | 8.18 |
| CHEMBL5948820 | — | — | 3 | 8.12 |
| CHEMBL5778223 | — | — | 3 | 8.12 |
| CHEMBL5950488 | — | — | 3 | 8.11 |
| CHEMBL5865451 | — | — | 3 | 8.09 |
| CHEMBL5863568 | — | — | 3 | 8.02 |
| CHEMBL5757312 | — | — | 3 | 8.00 |
| CHEMBL6057462 | — | — | 3 | 7.98 |
| CHEMBL5935960 | — | — | 3 | 7.97 |
| CHEMBL5801959 | — | — | 3 | 7.92 |
| CHEMBL6040007 | — | — | 3 | 7.89 |
| CHEMBL5972079 | — | — | 3 | 7.85 |
| CHEMBL5769037 | — | — | 3 | 7.85 |
| CHEMBL5926850 | — | — | 3 | 7.84 |
| CHEMBL5849962 | — | — | 3 | 7.82 |
| CHEMBL5947975 | — | — | 3 | 7.79 |
| CHEMBL5845465 | — | — | 3 | 7.77 |
| CHEMBL5949769 | — | — | 3 | 7.76 |
| CHEMBL5936570 | — | — | 3 | 7.75 |
| CHEMBL5943152 | — | — | 3 | 7.72 |
| CHEMBL5745822 | — | — | 3 | 7.72 |
| CHEMBL5985963 | — | — | 3 | 7.72 |
| CHEMBL5778189 | — | — | 3 | 7.68 |
| CHEMBL5813554 | — | — | 3 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5967615 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5757665 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5993886 | — | EC50 | = | 3.77 | nM | 8.42 |
| CHEMBL5977638 | — | EC50 | = | 5.11 | nM | 8.29 |
| CHEMBL5790478 | — | EC50 | = | 5.81 | nM | 8.24 |
| CHEMBL5992328 | — | EC50 | = | 5.91 | nM | 8.23 |
| CHEMBL6041191 | — | EC50 | = | 6.62 | nM | 8.18 |
| CHEMBL5948820 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5778223 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5950488 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5865451 | — | EC50 | = | 8.14 | nM | 8.09 |
| CHEMBL5863568 | — | EC50 | = | 9.57 | nM | 8.02 |
| CHEMBL5757312 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL6057462 | — | EC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5935960 | — | EC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5801959 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6040007 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5769037 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5972079 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5926850 | — | EC50 | = | 14.3 | nM | 7.84 |
| CHEMBL5849962 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5947975 | — | EC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5845465 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5949769 | — | EC50 | = | 17.3 | nM | 7.76 |
| CHEMBL5936570 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5985963 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5943152 | — | EC50 | = | 18.9 | nM | 7.72 |
| CHEMBL5745822 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5813554 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5778189 | — | EC50 | = | 20.7 | nM | 7.68 |
| CHEMBL5788562 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5960544 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5831527 | — | EC50 | = | 24.3 | nM | 7.61 |
| CHEMBL6049946 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5757520 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5747710 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5986883 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL6040035 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5772844 | — | EC50 | = | 29.6 | nM | 7.53 |
| CHEMBL5817643 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL5872235 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL6046238 | — | EC50 | = | 44.2 | nM | 7.36 |
| CHEMBL5977638 | — | EC50 | = | 64.7 | nM | 7.19 |
| CHEMBL5885144 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5862695 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5849169 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL6049858 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5787885 | — | EC50 | = | 84.8 | nM | 7.07 |
| CHEMBL5823588 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5765280 | — | EC50 | = | 104.0 | nM | 6.98 |