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Literature summary for 2.4.2.12 extracted from

  • Zhang, K.; Ni, Y.; Chen, J.; Tu, Z.; Wu, X.; Chen, D.; Yao, H.; Jiang, S.
    Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer (2019), Bioorg. Med. Chem. Lett., 29, 1502-1506 .
    View publication on PubMed
Search for more literature for 2.4.2.12

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-(pyridin-3-yl)-N-[6-(3-[[4-(trifluoromethyl)phenyl]sulfamoyl]phenyl)hexyl]prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(2,5-dimethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(2-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide most potent inhibitor Homo sapiens
(2E)-N-(6-[3-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(3-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-chlorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-ethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-phenoxyphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-(6-[3-[(4-tert-butylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[3-[3-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[3-[4-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[4-[4-(phenylsulfamoyl)phenyl]butyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[5-[3-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[5-[4-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[5-[4-([[2-(1H-indol-3-yl)ethyl](propan-2-yl)amino]methyl)anilino]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[6-[3-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[6-[4-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[7-[3-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
(2E)-N-[7-[4-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
-
 Homo sapiens
4-[[(3,7-dimethyl-4-oxo-3,4-dihydro-1,2,3-benzotriazin-6-yl)methyl](3-methylbut-2-en-1-yl)amino]-N-[(pyridin-3-yl)methyl]benzamide
-
 Homo sapiens
4-[[(4-tert-butylbenzene-1-sulfonyl)amino]methyl]-N-(pyridin-3-yl)benzamide
-
 Homo sapiens
6-[(benzylcarbamoyl)amino]-N-cyclohexyl-N-[2-(morpholin-4-yl)ethoxy]hexane-1-sulfonamide
-
 Homo sapiens
CHS828 also known as GMX1778 Homo sapiens
FK866
-
 Homo sapiens
N-([1,1'-biphenyl]-2-yl)-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide
-
 Homo sapiens
N-([4-[(3,5-difluorophenyl)methyl]phenyl]methyl)imidazo[1,2-a]pyridine-6-carboxamide
-
 Homo sapiens
N-[2-chloro-5-(trifluoromethyl)phenyl]-4-([[(pyridin-3-yl)methyl]carbamoyl]amino)benzene-1-sulfonamide
-
 Homo sapiens
N-[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]urea
-
 Homo sapiens
N-[4-(benzenesulfonyl)phenyl]-2-(pyridin-3-yl)cyclopropane-1-carboxamide
-
 Homo sapiens
N-[[4-(6-methylpyridine-3-sulfonyl)phenyl]methyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P43490
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
Huh-7 cell
-
 Homo sapiens
-
K-562 cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-
NCI-H1975 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Nampt
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000508
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(2-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.0000068
-
 pH and temperature not specified in the publication Homo sapiens FK866
0.0000092
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00000947
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-tert-butylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.0000097
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00000978
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00001053
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[6-[3-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
0.00001075
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-chlorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00001163
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(2,5-dimethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00001228
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(3-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00001309
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-phenoxyphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.00001442
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[6-[4-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
0.00001641
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[7-[4-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
0.00001654
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[5-[3-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
0.00001777
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[4-[4-(phenylsulfamoyl)phenyl]butyl]-3-(pyridin-3-yl)prop-2-enamide
0.00002453
-
 pH and temperature not specified in the publication Homo sapiens (2E)-3-(pyridin-3-yl)-N-[6-(3-[[4-(trifluoromethyl)phenyl]sulfamoyl]phenyl)hexyl]prop-2-enamide
0.00002839
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[5-[4-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
0.00003132
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[7-[3-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
0.00003154
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-(6-[3-[(4-ethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
0.0002345
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[3-[3-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
0.00592
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[3-[4-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide