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Literature summary for 2.7.11.10 extracted from

  • Al-Shaer, M.A.; Almazari, I.S.; Taha, M.O.
    Discovery of novel potent nuclear factor kappa-B inhibitors (IKK-beta) via extensive ligand-based modeling and virtual screening (2017), J. Mol. Recognit., 30, e2604 .
    View publication on PubMed
Search for more literature for 2.7.11.10

Inhibitors

Inhibitors Comment Organism Structure
1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline-6,7-diol NCI0288748, 65% inhibition at 0.1 mM Homo sapiens
1-[4-(1-hydroxynaphthalen-2-yl)-6-imino-3-methyl-6,7-dihydropyrazolo[3,4-d][1,3]thiazin-1(4H)-yl]-2-phenylethan-1-one NCI0657381, 76% inhibition at 0.1 mM Homo sapiens
2-[[bis(2-hydroxyethyl)amino]methyl]-4-(2-methylbutan-2-yl)phenol NCI0079692, 59% inhibition at 0.1 mM Homo sapiens
4-[6-[(2-hydroxyethyl)amino]-7-methyl-7,8-dihydro-2H,6H-[1,3]dioxolo[4,5-g][1]benzopyran-8-yl]-2,6-dimethoxyphenol NCI0671177, 68% inhibition at 0.1 mM Homo sapiens
4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide NCI0107328, 94% inhibition at 0.1 mM Homo sapiens
6,6-dimethyl-1-[3-[3-(3-nitrophenoxy)propoxy]phenyl]-1,3,5-triazinane-2,4-diimine NCI0111727, 75% inhibition at 0.1 mM Homo sapiens
7-(3-[[2-(3,5-dihydroxyphenyl)-2-hydroxyethyl]amino]propyl)-1,3-dimethyl-8-(morpholin-4-yl)-3,7-dihydro-1H-purine-2,6-dione NCI0293897, 55% inhibition at 0.1 mM Homo sapiens
lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide NCI0339925, 93% inhibition at 0.1 mM Homo sapiens
N-(3-[2-imino-6-methyl-3-[(3-nitrophenyl)methyl]-4-oxo-1,2,3,4-tetrahydropyrimidin-5-yl]propyl)-4-methylbenzene-1-sulfonamide NCI0211135, complete inhibition at 0.1 mM Homo sapiens
N2-(2-chlorophenyl)-N-[6-[(2-chlorophenyl)sulfamoyl]-2-methyl-4-oxoquinazolin-3(4H)-yl]glycinamide NCI0687760, 89% inhibition at 0.1 mM Homo sapiens
TPCA-1
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [IkappaB protein] Homo sapiens
-
 ADP + [IkappaB phosphoprotein]
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O14920
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast epithelial cell
-
 Homo sapiens
-
MCF-10A cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?

Synonyms

Synonyms Comment Organism
IKK-beta
-
 Homo sapiens
inhibitor kappa-B kinase-beta
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
 at 37°C, pH not specified in the publication Homo sapiens 4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide
0.00326
-
 at 37°C, pH not specified in the publication Homo sapiens N-(3-[2-imino-6-methyl-3-[(3-nitrophenyl)methyl]-4-oxo-1,2,3,4-tetrahydropyrimidin-5-yl]propyl)-4-methylbenzene-1-sulfonamide
0.01681
-
 at 37°C, pH not specified in the publication Homo sapiens lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide