Assay Detail
Binding
CHEMBL5370484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of biotinylated-H3K4me2 binding to N-terminal His9 tagged human BPTF isoform 2 PHD (2722 to 2781 residues) expressed in Escherichia coli BL21 Star (DE3) measured after 1 hr by Alphascreen assay
15
Total Activities
15
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
Nucleosome-remodeling factor subunit BPTF (CHEMBL3085621) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fragment-Based NMR Screening of the BPTF PHD Finger Methyl Lysine Reader Leads to the First Small-Molecule Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 3.74 | 4.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416607 | — | — | 1 | 4.70 |
| CHEMBL5432936 | — | — | 1 | 4.60 |
| CHEMBL4982613 | — | — | 1 | 4.52 |
| CHEMBL1632046 | — | — | 1 | 4.20 |
| CHEMBL1632047 | — | — | 1 | 3.89 |
| CHEMBL5418058 | — | — | 1 | 3.82 |
| CHEMBL5394921 | — | — | 1 | 3.66 |
| CHEMBL5414828 | — | — | 1 | 3.52 |
| CHEMBL5400051 | — | — | 1 | 3.42 |
| CHEMBL5394699 | — | — | 1 | 3.42 |
| CHEMBL1444734 | — | — | 1 | 3.30 |
| CHEMBL130880 | IPIDACRINE | 2.0 | 1 | 3.23 |
| CHEMBL127023 | — | — | 1 | 3.12 |
| CHEMBL5432787 | — | — | 1 | 2.92 |
| CHEMBL5407853 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416607 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5432936 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4982613 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1632046 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL1632047 | — | IC50 | = | 130000.0 | nM | 3.89 |
| CHEMBL5418058 | — | IC50 | = | 150000.0 | nM | 3.82 |
| CHEMBL5394921 | — | IC50 | = | 220000.0 | nM | 3.66 |
| CHEMBL5414828 | — | IC50 | = | 300000.0 | nM | 3.52 |
| CHEMBL5400051 | — | IC50 | = | 380000.0 | nM | 3.42 |
| CHEMBL5394699 | — | IC50 | = | 380000.0 | nM | 3.42 |
| CHEMBL1444734 | — | IC50 | = | 500000.0 | nM | 3.30 |
| CHEMBL130880 | IPIDACRINE | IC50 | = | 590000.0 | nM | 3.23 |
| CHEMBL127023 | — | IC50 | = | 750000.0 | nM | 3.12 |
| CHEMBL5432787 | — | IC50 | = | 1200000.0 | nM | 2.92 |
| CHEMBL5407853 | — | IC50 | - | — | - |