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Literature summary for 2.4.2.12 extracted from

  • Curtin, M.L.; Heyman, H.R.; Clark, R.F.; Sorensen, B.K.; Doherty, G.A.; Hansen, T.M.; Frey, R.R.; Sarris, K.A.; Aguirre, A.L.; Shrestha, A.; Tu, N.; Woller, K.; Pliushchev, M.A.; Sweis, R.F.; Cheng, M.; Wilsbacher, J.L.; Kovar, P.J.; Guo, J.; Cheng, D.; Longenecker, K.L.; Raich, D.; Korepanova, A.V.; Soni, N.B.; Algire, M.A.
    SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT) (2017), Bioorg. Med. Chem. Lett., 27, 3317-3325 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-chloro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5,6-dimethoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-(hydroxymethyl)-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-chloro-N-(4-[1-[(2S)-oxolane-2-carbonyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-cyano-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-fluoro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-fluoro-N-[4-[1-(1-methylpiperidine-4-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-fluoro-N-[4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-methoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
5-methyl-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
FK866
-
Homo sapiens
GMX1778
-
Homo sapiens
methyl 4-[(1,3-dihydro-2H-isoindole-2-carbonyl)amino]benzoate
-
Homo sapiens
N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-methylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-[1-[2-methyl-2-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-[[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-[[(oxan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-[[(oxolan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-(4-[[1-(2-methylbutanoyl)piperidin-4-yl]oxy]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-([4-[1-(oxan-4-yl)piperidine-4-sulfonyl]phenyl]methyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
Homo sapiens
N-[3-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(1-benzoylazetidin-3-yl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(benzenesulfonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-([[(3S)-oxolan-3-yl]methyl]carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3,3-dimethylbutyl)(methyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3,3-dimethylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
Homo sapiens
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3-methylbutyl)sulfamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(3-phenylpropyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[(4-methylpentanoyl)amino]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(3-methyloxetane-3-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[1-(cyclopropanesulfonyl)piperidin-4-yl]phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[4-[4-(pyridin-2-yl)piperazine-1-carbonyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[5-[(3-methylbutyl)carbamoyl]pyridin-2-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[6-[(3-methylbutyl)carbamoyl]pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens
N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
-
Homo sapiens
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P43490
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Nampt
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000015
-
N-(4-[1-[2-methyl-2-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000016
-
N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000017
-
5-chloro-N-(4-[1-[(2S)-oxolane-2-carbonyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000019
-
N-[4-(1-benzoylazetidin-3-yl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000025
-
5-fluoro-N-[4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000003
-
FK866 pH and temperature not specified in the publication Homo sapiens
0.000003
-
GMX1778 pH and temperature not specified in the publication Homo sapiens
0.000003
-
N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000039
-
N-[4-[1-(cyclopropanesulfonyl)piperidin-4-yl]phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000043
-
N-[4-[1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000047
-
5-cyano-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000049
-
5-(hydroxymethyl)-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000051
-
N-[4-[1-(3-methyloxetane-3-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000054
-
N-[5-[(3-methylbutyl)carbamoyl]pyridin-2-yl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000056
-
N-[4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000075
-
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000079
-
5-fluoro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000009
-
N-[4-[(3-phenylpropyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000094
-
5-fluoro-N-[4-[1-(1-methylpiperidine-4-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000011
-
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000013
-
5-methyl-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000013
-
N-(4-[[(oxan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000014
-
N-[4-[(3,3-dimethylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000014
-
N-[4-[4-(pyridin-2-yl)piperazine-1-carbonyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000015
-
N-[4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000016
-
5-methoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000017
-
4-chloro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000018
-
N-(4-[[1-(2-methylbutanoyl)piperidin-4-yl]oxy]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000019
-
N-(4-[[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000019
-
N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000019
-
N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000021
-
N-[4-(benzenesulfonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000023
-
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000023
-
N-[4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000024
-
N-(4-[[(oxolan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000057
-
N-[6-[(3-methylbutyl)carbamoyl]pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000058
-
N-[4-[(4-methylpentanoyl)amino]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000104
-
N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000112
-
methyl 4-[(1,3-dihydro-2H-isoindole-2-carbonyl)amino]benzoate pH and temperature not specified in the publication Homo sapiens
0.00016
-
N-[4-[(3,3-dimethylbutyl)(methyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00035
-
N-[4-[(3-methylbutyl)sulfamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000487
-
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00056
-
N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0022
-
N-(4-methylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0089
-
N-[3-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Ki above 0.0089 mM, pH and temperature not specified in the publication Homo sapiens
0.009
-
5,6-dimethoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Ki above 0.009 mM, pH and temperature not specified in the publication Homo sapiens