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Results 1 - 10 of 18 > >>
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EC Number Inhibitors Commentary Structure
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3661-methyl-5H-[1,2,4]triazolo[4,3-a][3,1]benzoxazine SETDB1-TTD inhibitor, binds to the acetyl lysine (Kac) pocket of the SETDB1-TTD Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3661-[(3,4-dimethoxyphenyl)methyl]-4-[[2-(trifluoromethyl)-7H-pyrrolo[2,3-b]pyridin-7-yl]methyl]piperidin-4-ol peptidecompetitive SETDB1 inhibitor, decreases SETDB1/ESET levels without changing the mRNA levels (FRET) and exerts noticeable inhibitory effects on H3K9 trimethylation. Induces neuronal cytotoxicity at 0.1 mM Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3662-([5-[4-(benzyloxy)phenyl]-1-methylpiperidin-3-yl]amino)-3-(prop-2-en-1-yl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one SETDB1-TTD inhibitor, inhibits the interaction of H3 peptide with the SETDB1-TTD Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3663,3-dimethyl-1-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-yl]butan-1-one SETDB1-TTD inhibitor, very weak binding in the aromatic cage of the dimethyl lysine (Kme2) pocket of the SETDB1-TTD Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3665-[(prop-2-en-1-yl)oxy]-2-(pyrrolidin-1-yl)quinoline SETDB1 SET domain inhibitor, inhibits SETDB1 activity and H3K9me3 expression, and improves motor function and neuropathological symptoms with minimal toxicity in mouse HD models Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.3667-chloro-2-[3-(dimethylamino)propyl]-1-(3-ethoxyphenyl)-1,2,3a,9a-tetrahydro[1]benzopyrano[2,3-c]pyrrole-3,9-dione peptidecompetitive SETDB1 inhibitor, decreases H3K9me3 levels and shows neuronal effects without cytotoxicity Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.366ATF7IP SETDB1 partner protein. SETDB1 and the SETDB1:ATF7IP complex efficiently catalyze both monomethylation and dimethylation of H3K9 peptide substrates. The activity of the binary complex is 4fold lower than SETDB1 alone Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.366N-[(furan-2-yl)methyl]-1-[(3S)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]piperidine-4-carboxamide SETDB1-TTD inhibitor, binds in the aromatic cage Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.366N-[2-(diethylamino)ethyl]-2-([5,7-dimethyl-6-[(2-methylphenyl)methyl][1,2,4]triazolo[1,5-a]pyrimidin-2-yl]sulfanyl)acetamide competitive SETDB1 inhibitor, decreases H3K9me3 levels and shows neuronal effects without cytotoxicity Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 2.1.1.366N-[[1,1'-bi(cyclohexan)]-4-yl]-6-methoxy-7-[3-(piperidin-1-yl)propoxy]-2-[4-(propan-2-yl)-1,4-diazepan-1-yl]quinazolin-4-amine competitive inhibition, the inhibitor docks in the Tudor domain Go to the Ligand Summary Page
Results 1 - 10 of 18 > >>
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