Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T86399 | Target Info | |||
| Target Name | Bromodomain-containing protein 2 (BRD2) | ||||
| Synonyms |
Really interesting new gene 3 protein; RING3; O27.1.1; KIAA9001
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| Target Type | Clinical trial Target | ||||
| Gene Name | BRD2 | ||||
| Biochemical Class | Bromodomain | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Bromodomain testis-specific protein (BRDT) | Clinical trial Target | ||||
| UniProt ID | BRDT_HUMAN | |||||
| Gene Name | BRDT | |||||
| Synonyms |
Cancer/testis antigen 9; CT9
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| Representative Drug(s) | ABBV-744 | Drug Info | Ki = 1 nM | [1] | ||
| Co-Target Name | Bromodomain-containing protein 4 (BRD4) | Clinical trial Target | ||||
| UniProt ID | BRD4_HUMAN | |||||
| Gene Name | BRD4 | |||||
| Synonyms |
Protein HUNK1; HUNK1
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| Representative Drug(s) | ABBV-744 | Drug Info | Ki = 1.6 nM | Click to Show More | [1] | |
| 2 | OTX-015 | Drug Info | Ki = 5.7 nM | [3] | ||
| Co-Target Name | Bromodomain-containing protein 3 (BRD3) | Clinical trial Target | ||||
| UniProt ID | BRD3_HUMAN | |||||
| Gene Name | BRD3 | |||||
| Synonyms |
RING3like protein; RING3L; RING3-like protein; KIAA0043
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| Representative Drug(s) | OTX-015 | Drug Info | Ki = 4 nM | Click to Show More | [2] | |
| 2 | ABBV-744 | Drug Info | Ki = 4.9 nM | [1] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H-pyrrolo[2,3- c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain. J Med Chem. 2020 May 28;63(10):5585-5623. | ||||
| REF 2 | Structure-Based Design of -Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. J Med Chem. 2015 Jun 25;58(12):4927-39. | ||||
| REF 3 | Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. | ||||
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