Assay Detail
Binding
CHEMBL5579970
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-carboxyfluorescein GpYLPQTV-NH2 probe from C-terminal 6His-tagged recombinant human STAT3 (127 to 711 residues) SH2 domain extracted from Escherichia coli BL21 (DE3) assessed as inhibition of dimerization preincubated for 60 mins followed by probe addition and measured after 30 mins by fluorescence polarization assay
11
Total Activities
11
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
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 | 11 | 5.02 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5594904 | — | — | 1 | 6.72 |
| CHEMBL1829876 | — | — | 1 | 5.28 |
| CHEMBL4746031 | — | — | 1 | 5.07 |
| CHEMBL4778873 | — | — | 1 | 5.01 |
| CHEMBL4795233 | — | — | 1 | 4.84 |
| CHEMBL1829786 | — | — | 1 | 4.70 |
| CHEMBL5592621 | — | — | 1 | 4.45 |
| CHEMBL5590435 | — | — | 1 | 4.08 |
| CHEMBL5595745 | — | — | 1 | - |
| CHEMBL5592262 | — | — | 1 | - |
| CHEMBL4764925 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5594904 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1829876 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4746031 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4778873 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4795233 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL1829786 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL5592621 | — | IC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL5590435 | — | IC50 | = | 82500.0 | nM | 4.08 |
| CHEMBL5595745 | — | IC50 | = | 180700.0 | nM | - |
| CHEMBL5592262 | — | IC50 | > | 600000.0 | nM | - |
| CHEMBL4764925 | — | IC50 | > | 600000.0 | nM | - |