Assay Detail
Binding
CHEMBL5330459
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human recombinant BRPF1B bromodomain using biotinylated H4 (1 to 21)K5/8/12/16Ac peptide as substrate incubated for 0.5 hrs by AlphaScreen assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Development of 3-acetylindole derivatives that selectively target BRPF1 as new inhibitors of receptor activator of NF-κB ligand (RANKL)-Induced osteoclastogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.42 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3356143 | — | — | 1 | 7.33 |
| CHEMBL5396399 | — | — | 1 | 7.16 |
| CHEMBL5426603 | — | — | 1 | 7.05 |
| CHEMBL5399573 | — | — | 1 | 6.99 |
| CHEMBL5418404 | — | — | 1 | 6.96 |
| CHEMBL5407472 | — | — | 1 | 6.96 |
| CHEMBL5421225 | — | — | 1 | 6.76 |
| CHEMBL5401348 | — | — | 1 | 6.69 |
| CHEMBL5421346 | — | — | 1 | 6.63 |
| CHEMBL5394845 | — | — | 1 | 6.53 |
| CHEMBL5424409 | — | — | 1 | 6.51 |
| CHEMBL5395880 | — | — | 1 | 6.36 |
| CHEMBL5436910 | — | — | 1 | 6.27 |
| CHEMBL5434261 | — | — | 1 | 6.25 |
| CHEMBL5410170 | — | — | 1 | 6.13 |
| CHEMBL5411385 | — | — | 1 | 6.04 |
| CHEMBL5407979 | — | — | 1 | 5.96 |
| CHEMBL5432139 | — | — | 1 | 5.95 |
| CHEMBL5401405 | — | — | 1 | 5.84 |
| CHEMBL5437588 | — | — | 1 | 5.77 |
| CHEMBL5423850 | — | — | 1 | 5.74 |
| CHEMBL5406426 | — | — | 1 | 5.46 |
| CHEMBL5393756 | — | — | 1 | - |
| CHEMBL5406791 | — | — | 1 | - |
| CHEMBL5422682 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3356143 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5396399 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5426603 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5399573 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5418404 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5407472 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5421225 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5401348 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5421346 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL5394845 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL5424409 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL5395880 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL5436910 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5434261 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL5410170 | — | IC50 | = | 743.0 | nM | 6.13 |
| CHEMBL5411385 | — | IC50 | = | 908.0 | nM | 6.04 |
| CHEMBL5407979 | — | IC50 | = | 1091.0 | nM | 5.96 |
| CHEMBL5432139 | — | IC50 | = | 1117.0 | nM | 5.95 |
| CHEMBL5401405 | — | IC50 | = | 1442.0 | nM | 5.84 |
| CHEMBL5437588 | — | IC50 | = | 1696.0 | nM | 5.77 |
| CHEMBL5423850 | — | IC50 | = | 1829.0 | nM | 5.74 |
| CHEMBL5406426 | — | IC50 | = | 3428.0 | nM | 5.46 |
| CHEMBL5393756 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406791 | — | IC50 | - | — | - | |
| CHEMBL5422682 | — | IC50 | - | — | - |