Assay Detail
Binding
CHEMBL5579965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant wild type tyrosine phosphorylated C-terminal 6His tagged human STAT3 C426A mutant (127 to 711 residues) DNA-binding activity transfected in v-Src transformed mouse NIH3T3 cell nuclear extract preincubated for 30 mins followed by addition of radiolabeled hSIE and measured after 30 mins by EMSA analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Subcellular | Nucleus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Signal transducer and activator of transcription 3 (CHEMBL4026) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.93 | 5.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592262 | — | — | 1 | 5.22 |
| CHEMBL4764925 | — | — | 1 | 5.12 |
| CHEMBL1829876 | — | — | 1 | 4.97 |
| CHEMBL4778873 | — | — | 1 | 4.70 |
| CHEMBL4746031 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592262 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4764925 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL1829876 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4778873 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4746031 | — | IC50 | = | 23000.0 | nM | 4.64 |