Assay Detail
Binding
CHEMBL4182259
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Binding affinity to His-tagged BRD2 bromodomain 2 (unknown origin) by SPR assay
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 | 7.10 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209110 | — | — | 1 | 7.33 |
| CHEMBL4205876 | — | — | 1 | 7.21 |
| CHEMBL4210405 | — | — | 1 | 7.14 |
| CHEMBL4202664 | — | — | 1 | 7.13 |
| CHEMBL4206677 | — | — | 1 | 7.11 |
| CHEMBL1957266 | — | — | 1 | 6.94 |
| CHEMBL4207106 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209110 | — | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL4205876 | — | Kd | = | 61.0 | nM | 7.21 |
| CHEMBL4210405 | — | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL4202664 | — | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL4206677 | — | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL1957266 | — | Kd | = | 116.0 | nM | 6.94 |
| CHEMBL4207106 | — | Kd | = | 148.0 | nM | 6.83 |