Assay Detail
Binding
CHEMBL4182262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to BRD2 bromodomain 2 (348 to 455 residues) (unknown origin) by ITC
7
Total Activities
7
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 |
|---|---|---|---|
| Kd | 7 | 7.23 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210405 | — | — | 1 | 7.77 |
| CHEMBL4206677 | — | — | 1 | 7.70 |
| CHEMBL4205876 | — | — | 1 | 7.68 |
| CHEMBL4202664 | — | — | 1 | 7.45 |
| CHEMBL1957266 | — | — | 1 | 6.95 |
| CHEMBL4209110 | — | — | 1 | 6.55 |
| CHEMBL4207106 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210405 | — | Kd | = | 17.12 | nM | 7.77 |
| CHEMBL4206677 | — | Kd | = | 19.94 | nM | 7.70 |
| CHEMBL4205876 | — | Kd | = | 20.87 | nM | 7.68 |
| CHEMBL4202664 | — | Kd | = | 35.86 | nM | 7.45 |
| CHEMBL1957266 | — | Kd | = | 112.14 | nM | 6.95 |
| CHEMBL4209110 | — | Kd | = | 280.44 | nM | 6.55 |
| CHEMBL4207106 | — | Kd | = | 299.51 | nM | 6.52 |