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Literature summary extracted from

  • Wu, J.P.; Fleck, R.; Brickwood, J.; Capolino, A.; Catron, K.; Chen, Z.; Cywin, C.; Emeigh, J.; Foerst, M.; Ginn, J.; Hrapchak, M.; Hickey, E.; Hao, M.H.; Kashem, M.; Li, J.; Liu, W.; Morwick, T.; Nelson, R.; Marshall, D.; Martin, L.; Nemoto, P.; Potocki, I.; Liuzzi, M.; Peet, G.W.; Scouten, E.; Stefany, D.; Turner, M.; Weldon, S.; Zimmitti, C.; Spero, D.; Kelly, T.A.
    The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II (2009), Bioorg. Med. Chem. Lett., 19, 5547-5551.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.10 medicine IKKbeta inhibitors are utilized for the treatment of cancer and immunological disorders Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.10 3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-hydroxy-3,3-dimethylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.10 methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.10 Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IkappaB kinase
-
 Homo sapiens
2.7.11.10 IKK
-
 Homo sapiens
2.7.11.10 IKKbeta one of the catalytic subunits Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.10 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.10 0.000041
-
 IKKbeta Homo sapiens 3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.000072
-
 IKKbeta Homo sapiens 3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00009
-
 IKKalpha Homo sapiens 3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.000098
-
 IKKbeta Homo sapiens 3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00012
-
 IKKbeta Homo sapiens 3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00012
-
 IKKbeta Homo sapiens 3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00014
-
 IKKbeta Homo sapiens 3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00015
-
 IKKbeta Homo sapiens 3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00028
-
 IKKbeta Homo sapiens 3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0005
-
 IKKbeta Homo sapiens 3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00052
-
 IKKbeta Homo sapiens 3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00057
-
 IKKbeta Homo sapiens 3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00059
-
 IKKbeta Homo sapiens 3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00063
-
 IKKbeta Homo sapiens 3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00068
-
 IKKbeta Homo sapiens 3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00068
-
 IKKbeta Homo sapiens 3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00068
-
 IKKbeta Homo sapiens 3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00075
-
 IKKbeta Homo sapiens 3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0011
-
 IKKbeta Homo sapiens 3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0013
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0013
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0013
-
 IKKbeta Homo sapiens 3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00145
-
 IKKbeta Homo sapiens 3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0016
-
 whole blood assay Homo sapiens 3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.00195
-
 IKKbeta Homo sapiens 3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.002
-
 IKKbeta Homo sapiens 3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.002
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.002
-
 IKKbeta Homo sapiens 3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0022
-
 IKKbeta Homo sapiens 3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0024
-
 IKKbeta Homo sapiens 3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0024
-
 IKKbeta Homo sapiens 3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0025
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0025
-
 IKKbeta Homo sapiens 3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0027
-
 IKKbeta Homo sapiens 3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0029
-
 IKKbeta Homo sapiens 3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0032
-
 whole blood assay Homo sapiens 3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0034
-
 IKKalpha Homo sapiens 3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0047
-
 IKKbeta Homo sapiens 3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0051
-
 IKKbeta Homo sapiens 3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0058
-
 IKKbeta Homo sapiens 3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.006
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0066
-
 IKKbeta Homo sapiens 3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0074
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0078
-
 IKKbeta Homo sapiens methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
2.7.11.10 0.0085
-
 IKKbeta Homo sapiens 3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0098
-
 whole blood assay Homo sapiens 3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0108
-
 IKKbeta Homo sapiens 3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0112
-
 IKKalpha Homo sapiens 3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0127
-
 IKKbeta Homo sapiens 3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.013
-
 whole blood assay Homo sapiens 3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0133
-
 IKKalpha Homo sapiens 3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.014
-
 IKKbeta Homo sapiens 3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.0169
-
 IKKbeta Homo sapiens 3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.02
-
 IKKbeta, larger than 0.0200 Homo sapiens 3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
2.7.11.10 0.05
-
 IKKbeta, larger than 0.0500 Homo sapiens 3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide

General Information

EC Number General Information Comment Organism
2.7.11.10 physiological function the IkappaB kinase complex is critical for the activation of the NF-kappaB pathway Homo sapiens