Assay Detail
Binding
CHEMBL5317208
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Binding affinity to human his-tagged recombinant YEATS4 expressed in Escherichia coli assessed as inhibition constant using biotin tagged lysine 27-crotonylated histone H3 peptide as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by FRET analysis
13
Total Activities
13
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
YEATS domain-containing protein 4 (CHEMBL4296266) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.17 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5397585 | — | — | 1 | 7.68 |
| CHEMBL5414722 | — | — | 1 | 7.48 |
| CHEMBL5428051 | — | — | 1 | 7.48 |
| CHEMBL5439842 | — | — | 1 | 7.43 |
| CHEMBL5432565 | — | — | 1 | 7.37 |
| CHEMBL5439506 | — | — | 1 | 7.25 |
| CHEMBL5426169 | — | — | 1 | 7.24 |
| CHEMBL5434894 | — | — | 1 | 7.23 |
| CHEMBL5411016 | — | — | 1 | 7.20 |
| CHEMBL5432083 | — | — | 1 | 7.16 |
| CHEMBL5429949 | — | — | 1 | 6.85 |
| CHEMBL5435884 | — | — | 1 | 6.55 |
| CHEMBL5439514 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5397585 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5414722 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5428051 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5439842 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL5432565 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL5439506 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL5426169 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL5434894 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5411016 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL5432083 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL5429949 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL5435884 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL5439514 | — | Ki | = | 540.0 | nM | 6.27 |