Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T90985 | Target Info | |||
| Target Name | Bromodomain testis-specific protein (BRDT) | ||||
| Synonyms |
Cancer/testis antigen 9; CT9
Click to Show/Hide
|
||||
| Target Type | Clinical trial Target | ||||
| Gene Name | BRDT | ||||
| Biochemical Class | Bromodomain | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4207347
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50458954
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 50000 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3590383; BDBM50098301; YD4
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 50118.72 nM
|
[2] | |||
| Compound Name |
4-(2,5-Dimethoxyphenyl)-3-methyl-5-propyl-2,4-dihydropyrrolo[3,4-c]pyrrol-6-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4066897
Click to Show/Hide
|
||||
| Activity |
IC50 = 67000 nM
|
[3] | |||
| Compound Name |
7-(4-Fluorobenzyl)-3-methyl-8-(methylamino)-1H-purine-2,6(3H,7H)-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
Oprea1_261894; Oprea1_475857; CHEMBL4098168; ZINC119685; AKOS024601641; MCULE-9092452578; EU-0043644; AB00672844-01; F0887-0152
Click to Show/Hide
|
||||
| Activity |
IC50 = 68000 nM
|
[3] | |||
| Compound Name |
8-(2-Hydroxyethylamino)-7-(naphthalen-1-ylmethyl)-3H-purine-2,6-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4101588
Click to Show/Hide
|
||||
| Activity |
IC50 = 87000 nM
|
[3] | |||
| 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774931; SCHEMBL19066319; BDBM50150069; ZINC68716836; AKOS008738479; MCULE-3915679099; J3.601.437G; Q27455888; Z642854042
Click to Show/Hide
|
||||
| Activity |
IC50 = 100000 nM
|
[4] | |||
| Compound Name |
8-[(5-Amino-1H-1,2,4-triazol-3-yl)sulfanylmethyl]-3-[(4-chlorophenyl)methyl]-7-ethylpurine-2,6-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3774900; SCHEMBL19066325; BDBM50150752
Click to Show/Hide
|
||||
| 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
Click to Show/Hide
|
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
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(E)-N'-Methoxy-N-[7-(pyridin-3-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl]methanimidamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4059728; AKOS005077827; MCULE-9789429399; 11K-060
Click to Show/Hide
|
||||
| Activity |
IC50 = 120000 nM
|
[3] | |||
| Compound Name |
5-(2-Furyl)-1-(tetrahydro-2-furanylmethyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4080143; STK626126; AKOS003070077; AKOS005559378; MCULE-3687410212; 5-(furan-2-yl)-1-((tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione; 5-(furan-2-yl)-2-hydroxy-1-(tetrahydrofuran-2-ylmethyl)pyrido[2,3-d]pyrimidin-4(1H)-one
Click to Show/Hide
|
||||
| Activity |
IC50 = 130000 nM
|
[3] | |||
| Compound Name |
1,3-Diethyl-2-oxo-2,3-dihydro-1H-benzoimidazole-5-carbaldehyde
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
1,3-diethyl-2-oxobenzimidazole-5-carbaldehyde; 1,3-diethyl-2-oxo-2,3-dihydro-1H-benzimidazole-5-carbaldehyde; 1,3-diethyl-2-oxo-2,3-dihydro-1H-1,3-benzodiazole-5-carbaldehyde; 1,3-diethyl-2-oxo-3-hydrobenzimidazole-5-carbaldehyde; SCHEMBL5836360; CHEMBL4094383; CTK7H9824; ZINC4384219; BBL022528; MFCD07643203; SBB011376; STL259660; AKOS000103825; MCULE-4744378422; ST076736; VS-07218; BB 0217060; 1,3-Diethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carbaldehyde; 1,3-Diethyl-2-oxo-2,3-dihydro-1H-benzimidazole-5-carbaldehyde, AldrichCPR
Click to Show/Hide
|
||||
| Activity |
IC50 = 140000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5-Ethyl-5-methyl-5,6-dihydrobenzo[h]quinazolin-4(3H)-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
MLS001213485; CHEMBL1471174; HMS2883A19; STK558694; AKOS005484475; MCULE-3078830963; SMR000540514; 5-methyl-5-ethyl-4-oxo-3,4,5,6-tetrahydrobenzo[h]quinazoline
Click to Show/Hide
|
||||
| Activity |
IC50 = 220000 nM
|
[3] | |||
| Compound Name |
8-Chloro-6-(4-chlorophenyl)-1-methyl-3H,4H-benzo[g]1,5-diazocin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4088018; ZINC18322710; AKOS002320500; ST50759579
Click to Show/Hide
|
||||
| Activity |
IC50 = 220000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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. | ||||
| REF 2 | Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. J Med Chem. 2015 Aug 13;58(15):6151-78. | ||||
| REF 3 | BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. J Med Chem. 2017 Jun 22;60(12):4805-4817. | ||||
| REF 4 | 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 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. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.