Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T42048 | Target Info | |||
| Target Name | Bromodomain-containing protein 3 (BRD3) | ||||
| Synonyms |
RING3like protein; RING3L; RING3-like protein; KIAA0043
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| Target Type | Clinical trial Target | ||||
| Gene Name | BRD3 | ||||
| Biochemical Class | Bromodomain | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
I-BRD9
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|
Investigative | Compound Info | ||
| Synonyms |
GSK602; compound 45 [PMID 25856009]
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| Activity |
IC50 ~ 50118.72 nM
|
[1] | |||
| Compound Name |
8-[[(3R,4R)-3-[(1,1-Dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3590383; BDBM50098301; YD4
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| Activity |
IC50 ~ 50118.72 nM
|
[2] | |||
| Compound Name |
3-Butyl-8-[(6-Butyl-5,7-Dimethyl-[1,2,4]triazolo[1,5-A]pyrimidin-2-Yl)sulfanylmethyl]-7-Ethyl-Purine-2,6-Dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774931; SCHEMBL19066319; BDBM50150069; ZINC68716836; AKOS008738479; MCULE-3915679099; J3.601.437G; Q27455888; Z642854042
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| Activity |
IC50 = 62000 nM
|
[3] | |||
| Compound Name |
Ethyl N-[(4S)-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]carbamate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2430872; BDBM50441169
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| Activity |
IC50 = 100000 nM
|
[4] | |||
| Compound Name |
2-(4-Hydroxy-3,5-Dimethylphenyl)-7-Methyl-5,6,7,8-Tetrahydropyrido[4',3':4,5]thieno[2,3-D]pyrimidin-4(3h)-One
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Investigative | Compound Info | ||
| Synonyms |
FL-411; CHEMBL4077274; BRD4-IN-1; FL411; SCHEMBL22374551; EX-A3383; BDBM50251045; FL 411; s1027; FL-411,; BS-16486; HY-111102; AK00779493; CS-0034229
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39. | ||||
| REF 2 | Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. J Med Chem. 2015 Aug 13;58(15):6151-78. | ||||
| REF 3 | Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins. J Med Chem. 2016 Feb 25;59(4):1634-41. | ||||
| REF 4 | Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem. 2013 Oct 10;56(19):7501-15. | ||||
| REF 5 | Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. J Med Chem. 2017 Dec 28;60(24):9990-10012. | ||||
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