Assay Detail
Binding
CHEMBL4144033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged Brd3 bromodomain 1 expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of biotinylated acetyl-histone H4 peptide and measured after 1 hr by AlphaScreen assay
23
Total Activities
23
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 |
Publication
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.74 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4168815 | — | — | 1 | 8.05 |
| CHEMBL4177080 | — | — | 1 | 8.00 |
| CHEMBL4173305 | — | — | 1 | 8.00 |
| CHEMBL4170756 | — | — | 1 | 7.96 |
| CHEMBL4162832 | — | — | 1 | 7.92 |
| CHEMBL4159455 | — | — | 1 | 7.89 |
| CHEMBL4176902 | — | — | 1 | 7.89 |
| CHEMBL4169698 | — | — | 1 | 7.85 |
| CHEMBL4176672 | — | — | 1 | 7.85 |
| CHEMBL4166861 | — | — | 1 | 7.80 |
| CHEMBL4174764 | — | — | 1 | 7.75 |
| CHEMBL4164698 | — | — | 1 | 7.72 |
| CHEMBL2132936 | — | — | 1 | 7.72 |
| CHEMBL4166286 | — | — | 1 | 7.68 |
| CHEMBL4174587 | — | — | 1 | 7.68 |
| CHEMBL4174918 | — | — | 1 | 7.68 |
| CHEMBL4173537 | — | — | 1 | 7.64 |
| CHEMBL4169877 | — | — | 1 | 7.60 |
| CHEMBL4166455 | — | — | 1 | 7.44 |
| CHEMBL4166671 | — | — | 1 | 7.41 |
| CHEMBL4162818 | — | — | 1 | 7.36 |
| CHEMBL4161952 | — | — | 1 | 7.28 |
| CHEMBL4160537 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4168815 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4177080 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4173305 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4170756 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4162832 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4159455 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4176902 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4169698 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4176672 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4166861 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4174764 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4164698 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2132936 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4166286 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4174587 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4174918 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4173537 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4169877 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4166455 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4166671 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4162818 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4161952 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4160537 | — | IC50 | > | 10000.0 | nM | - |