Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T40556 | Target Info | |||
| Target Name | Bromodomain-containing protein 4 (BRD4) | ||||
| Synonyms |
Protein HUNK1; HUNK1
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| Target Type | Clinical trial Target | ||||
| Gene Name | BRD4 | ||||
| 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 | Click to Show More | [1] | |
| 2 | AZD5153 | Drug Info | Ki = 100 nM | [5] | ||
| 3 | (+)-JQ1 | Drug Info | IC50 = 103 nM | [6] | ||
| 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] | ||
| 3 | (+)-JQ1 | Drug Info | Ki = 6.6 nM | [2] | ||
| 4 | GSK525762 | Drug Info | Ki = 30.3 nM | [2] | ||
| 5 | AZD5153 | Drug Info | Ki = 63.1 nM | [5] | ||
| Co-Target Name | Bromodomain-containing protein 2 (BRD2) | Clinical trial Target | ||||
| UniProt ID | BRD2_HUMAN | |||||
| Gene Name | BRD2 | |||||
| Synonyms |
Really interesting new gene 3 protein; RING3; O27.1.1; KIAA9001
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| Representative Drug(s) | ABBV-744 | Drug Info | Ki = 4.6 nM | Click to Show More | [1] | |
| 2 | OTX-015 | Drug Info | Ki = 5.4 nM | [3] | ||
| 3 | (+)-JQ1 | Drug Info | Ki = 12.5 nM | [2] | ||
| 4 | GSK525762 | Drug Info | IC50 = 32.5 nM | [4] | ||
| 5 | AZD5153 | Drug Info | Ki = 100 nM | [5] | ||
| 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 a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-81. | ||||
| REF 4 | Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem. 2011 Jun 9;54(11):3827-38. | ||||
| REF 5 | Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153). J Med Chem. 2016 Sep 8;59(17):7801-17. | ||||
| REF 6 | Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. J Med Chem. 2018 Sep 13;61(17):7785-7795. | ||||
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