Assay Detail
Binding
CHEMBL4828223
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Inhibition of HIS9-tagged BPTF (unknown origin) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by AlphaScreen assay
26
Total Activities
26
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
New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.98 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861491 | — | — | 1 | 7.44 |
| CHEMBL4848701 | — | — | 1 | 7.25 |
| CHEMBL4872300 | — | — | 1 | 7.17 |
| CHEMBL4848138 | — | — | 1 | 6.77 |
| CHEMBL4101756 | — | — | 1 | 6.66 |
| CHEMBL4850516 | — | — | 1 | 6.60 |
| CHEMBL4866748 | — | — | 1 | 6.54 |
| CHEMBL4870218 | — | — | 1 | 6.51 |
| CHEMBL4848082 | — | — | 1 | 6.43 |
| CHEMBL4863631 | — | — | 1 | 6.42 |
| CHEMBL4877696 | — | — | 1 | 6.26 |
| CHEMBL4850913 | — | — | 1 | 6.16 |
| CHEMBL4855881 | — | — | 1 | 6.10 |
| CHEMBL4863529 | — | — | 1 | 6.10 |
| CHEMBL4065579 | — | — | 1 | 6.02 |
| CHEMBL4877118 | — | — | 1 | 6.01 |
| CHEMBL4069412 | — | — | 1 | 5.82 |
| CHEMBL4861822 | — | — | 1 | 5.50 |
| CHEMBL4858548 | — | — | 1 | 5.41 |
| CHEMBL4872107 | — | — | 1 | 5.11 |
| CHEMBL4853420 | — | — | 1 | 5.06 |
| CHEMBL4849136 | — | — | 1 | 5.00 |
| CHEMBL4867912 | — | — | 1 | 5.00 |
| CHEMBL4857332 | — | — | 1 | 4.96 |
| CHEMBL4072538 | — | — | 1 | 4.72 |
| CHEMBL4871852 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861491 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4848701 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4872300 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4848138 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4101756 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4850516 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4866748 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4870218 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4848082 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4863631 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4877696 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4850913 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4855881 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4863529 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4065579 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4877118 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4069412 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4861822 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4858548 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4872107 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4853420 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4849136 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4867912 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4857332 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4072538 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4871852 | — | IC50 | = | 31000.0 | nM | 4.51 |