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Literature summary for 2.7.11.10 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
Search for more literature for 2.7.11.10

Application

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

Inhibitors

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

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
IkappaB kinase
-
 Homo sapiens
IKK
-
 Homo sapiens
IKKbeta one of the catalytic subunits Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

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

General Information

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