Assay Detail
Binding
CHEMBL4182256
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human BRD2 bromodomain 2 (342 to 460 residues) using biotin labeled peptide substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by TR-FRET assay
8
Total Activities
8
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
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.31 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177300 | — | — | 1 | 7.52 |
| CHEMBL1957266 | — | — | 1 | 6.77 |
| CHEMBL4206677 | — | — | 1 | 6.39 |
| CHEMBL4209110 | — | — | 1 | 6.21 |
| CHEMBL4205876 | — | — | 1 | 6.08 |
| CHEMBL4210405 | — | — | 1 | 5.97 |
| CHEMBL4202664 | — | — | 1 | 5.85 |
| CHEMBL4207106 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177300 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1957266 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4206677 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4209110 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4205876 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4210405 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4202664 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4207106 | — | IC50 | = | 1910.0 | nM | 5.72 |