Assay Detail
Binding
CHEMBL4144031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged Brd2 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
29
Total Activities
29
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 | 29 | 7.10 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4165389 | — | — | 1 | 8.22 |
| CHEMBL2132936 | — | — | 1 | 7.58 |
| CHEMBL4168815 | — | — | 1 | 7.48 |
| CHEMBL4161767 | — | — | 1 | 7.47 |
| CHEMBL4177080 | — | — | 1 | 7.46 |
| CHEMBL4170756 | — | — | 1 | 7.42 |
| CHEMBL4167362 | — | — | 1 | 7.36 |
| CHEMBL4162832 | — | — | 1 | 7.29 |
| CHEMBL4159455 | — | — | 1 | 7.28 |
| CHEMBL4173305 | — | — | 1 | 7.28 |
| CHEMBL4174587 | — | — | 1 | 7.27 |
| CHEMBL4173105 | — | — | 1 | 7.25 |
| CHEMBL4176672 | — | — | 1 | 7.19 |
| CHEMBL4176902 | — | — | 1 | 7.17 |
| CHEMBL4169698 | — | — | 1 | 7.10 |
| CHEMBL4173537 | — | — | 1 | 7.02 |
| CHEMBL4174764 | — | — | 1 | 6.94 |
| CHEMBL4169877 | — | — | 1 | 6.89 |
| CHEMBL4174918 | — | — | 1 | 6.89 |
| CHEMBL4166286 | — | — | 1 | 6.87 |
| CHEMBL4166671 | — | — | 1 | 6.82 |
| CHEMBL4166861 | — | — | 1 | 6.73 |
| CHEMBL4165200 | — | — | 1 | 6.69 |
| CHEMBL4164698 | — | — | 1 | 6.58 |
| CHEMBL4161952 | — | — | 1 | 6.56 |
| CHEMBL4162818 | — | — | 1 | 6.47 |
| CHEMBL4166455 | — | — | 1 | 6.41 |
| CHEMBL4167034 | — | — | 1 | - |
| CHEMBL4160537 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4165389 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2132936 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL4168815 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4161767 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4177080 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4170756 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4167362 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4162832 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4159455 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4173305 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4174587 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4173105 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4176672 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4176902 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4169698 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4173537 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4174764 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4169877 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4174918 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4166286 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4166671 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4166861 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4165200 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL4164698 | — | IC50 | = | 263.5 | nM | 6.58 |
| CHEMBL4161952 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4162818 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4166455 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL4167034 | — | IC50 | > | 999.0 | nM | - |
| CHEMBL4160537 | — | IC50 | > | 10000.0 | nM | - |