Assay Detail
Binding
CHEMBL5045539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human STING G230A/R293Q double mutant cytoplasmic domain (155 to 341 residues) assessed as induction of protein dimerization incubated for 1 hr by time-resolved FRET-based assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Stimulator of interferon genes protein (CHEMBL4523377) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Non-Nucleotide Small-Molecule STING Agonists <i>via</i> Chemotype Hybridization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 5.15 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438309 | — | — | 1 | 7.96 |
| CHEMBL4776666 | — | — | 1 | 7.21 |
| CHEMBL5091795 | — | — | 1 | 5.60 |
| CHEMBL5080916 | — | — | 1 | 5.31 |
| CHEMBL5082881 | — | — | 1 | 5.23 |
| CHEMBL5081567 | — | — | 1 | 5.22 |
| CHEMBL4528146 | — | — | 1 | 4.77 |
| CHEMBL5090440 | — | — | 1 | 4.75 |
| CHEMBL5082707 | — | — | 1 | 4.58 |
| CHEMBL5077683 | — | — | 1 | 4.50 |
| CHEMBL5082361 | — | — | 1 | 4.43 |
| CHEMBL5089143 | — | — | 1 | 4.30 |
| CHEMBL5092039 | — | — | 1 | 4.19 |
| CHEMBL5088178 | — | — | 1 | 4.08 |
| CHEMBL71263 | VADIMEZAN | 3.0 | 1 | - |
| CHEMBL5079595 | — | — | 1 | - |
| CHEMBL5086226 | — | — | 1 | - |
| CHEMBL5086556 | — | — | 1 | - |
| CHEMBL5076859 | — | — | 1 | - |
| CHEMBL5082150 | — | — | 1 | - |
| CHEMBL5078116 | — | — | 1 | - |
| CHEMBL5089074 | — | — | 1 | - |
| CHEMBL5088451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438309 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4776666 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5091795 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5080916 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5082881 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5081567 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4528146 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5090440 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL5082707 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5077683 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL5082361 | — | EC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL5089143 | — | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5092039 | — | EC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL5088178 | — | EC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL71263 | VADIMEZAN | EC50 | > | 100000.0 | nM | - |
| CHEMBL5079595 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5086226 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5086556 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5076859 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5082150 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5078116 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5089074 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5088451 | — | EC50 | > | 100000.0 | nM | - |