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Literature summary extracted from

  • Zheng, X.; Bair, K.W.; Bauer, P.; Baumeister, T.; Bowman, K.K.; Buckmelter, A.J.; Caligiuri, M.; Clodfelter, K.H.; Feng, Y.; Han, B.; Ho, Y.C.; Kley, N.; Li, H.; Liang, X.; Liederer, B.M.; Lin, J.; Ly, J.; OBrien, T.; Oeh, J.; Oh, A.; Reynolds, D.J.; Sampath, D.; Sharma, G.; Skelton, N.; Smith, C.C.; Tremayne, J.
    Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT) (2013), Bioorg. Med. Chem. Lett., 23, 5488-5497.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.12 1-methyl-N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 APO-866
-
 Homo sapiens
2.4.2.12 GMX-1777
-
 Homo sapiens
2.4.2.12 GMX-1778
-
 Homo sapiens
2.4.2.12 N-(4-[[1-(propan-2-yl)-1H-pyrazol-4-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-(4-[[3-(trifluoromethoxy)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-(4-[[3-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-(4-[[5-(trifluoromethyl)pyridin-3-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-([4-[4-(oxetan-3-yl)piperazine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-([4-[4-(pyrrolidin-1-yl)piperidine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-([4-[6-(dimethylamino)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(morpholin-4-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(phenylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-indazole-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(piperidin-1-ylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(quinolin-3-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(1-ethyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(1-propyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(4-cyanopiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(4-hydroxypiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[(5-chloropyridin-3-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[[4-(4-aminopiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[[4-(4-methoxypiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[[4-(7-oxa-2-azaspiro[3.5]nonane-2-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
2.4.2.12 N-[[4-(benzenesulfonyl)phenyl]methyl]-1H-pyrazolo[4,3-b]pyridine-5-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.12 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate Homo sapiens
-
 nicotinamide D-ribonucleotide + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.12 Homo sapiens P43490
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.12 A-2780 cell
-
 Homo sapiens
-
2.4.2.12 Calu-6 cell
-
 Homo sapiens
-
2.4.2.12 HCT-116 cell
-
 Homo sapiens
-
2.4.2.12 HT-1080 cell
-
 Homo sapiens
-
2.4.2.12 MiaPaCa cell
-
 Homo sapiens
-
2.4.2.12 PC-3 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.12 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 Homo sapiens nicotinamide D-ribonucleotide + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.12 Nampt
-
 Homo sapiens
2.4.2.12 PBEF
-
 Homo sapiens
2.4.2.12 pre-B cell colony-enhancing factor
-
 Homo sapiens
2.4.2.12 Visfatin
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.12 0.0000045
-
 pH and temperature not specified in the publication Homo sapiens N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0000061
-
 pH and temperature not specified in the publication Homo sapiens N-(4-[[3-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0000077
-
 pH and temperature not specified in the publication Homo sapiens N-(4-[[3-(trifluoromethoxy)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0000079
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0000082
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(quinolin-3-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00001
-
 pH and temperature not specified in the publication Homo sapiens N-(4-[[5-(trifluoromethyl)pyridin-3-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00001
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(1-propyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.000011
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(5-chloropyridin-3-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.000012
-
 pH and temperature not specified in the publication Homo sapiens N-([4-[6-(dimethylamino)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.000066
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.000088
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.000099
-
 pH and temperature not specified in the publication Homo sapiens N-(4-[[1-(propan-2-yl)-1H-pyrazol-4-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00011
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(7-oxa-2-azaspiro[3.5]nonane-2-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00019
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(1-ethyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0003
-
 pH and temperature not specified in the publication Homo sapiens N-([4-[4-(pyrrolidin-1-yl)piperidine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00037
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(morpholin-4-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00039
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(4-aminopiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0004
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(4-methoxypiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00041
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(4-cyanopiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00041
-
 pH and temperature not specified in the publication Homo sapiens N-[4-[(4-hydroxypiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.00044
-
 pH and temperature not specified in the publication Homo sapiens N-([4-[4-(oxetan-3-yl)piperazine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.0013
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(benzenesulfonyl)phenyl]methyl]-1H-pyrazolo[4,3-b]pyridine-5-carboxamide
2.4.2.12 0.002
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-indazole-5-carboxamide
2.4.2.12 0.002
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide
2.4.2.12 0.002
-
 pH and temperature not specified in the publication Homo sapiens 1-methyl-N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
2.4.2.12 0.002
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
2.4.2.12 0.018
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
2.4.2.12 0.028
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(piperidin-1-ylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide