Pub. Date : 2016 Nov
PMID : 27573426
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Herein, we report AZD5153, a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode. | AZD5153 | bromodomain containing 4 | Homo sapiens |
| 2 | Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. | AZD5153 | bromodomain containing 4 | Homo sapiens |
| 3 | The relationship between AZD5153 exposure and efficacy suggests that prolonged BRD4 target coverage is a primary efficacy driver. | AZD5153 | bromodomain containing 4 | Homo sapiens |
| 4 | This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies. | AZD5153 | bromodomain containing 4 | Homo sapiens |