BRENDA - Enzyme Database show

Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors

Zheng, X.; Bauer, P.; Baumeister, T.; Buckmelter, A.J.; Caligiuri, M.; Clodfelter, K.H.; Han, B.; Ho, Y.C.; Kley, N.; Lin, J.; Reynolds, D.J.; Sharma, G.; Smith, C.C.; Wang, Z.; Dragovich, P.S.; Gunzner-Toste, J.; Liederer, B.M.; Ly, J.; OBrien, T.; Oh, A.; Wang, L.; Wang, W.; Xiao, Y.; Zak, M.; Zhao, G.; Yue, Y.u.e.n.; J. Med. Chem. 56, 6413-6433 (2013)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.4.2.12
1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
Homo sapiens
2.4.2.12
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
-
Homo sapiens
2.4.2.12
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
-
Homo sapiens
2.4.2.12
FK866
i.e. (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
2.4.2.12
GMX-1778
i.e. (E)-1-(6-(4-chlorophenoxy)hexyl)-2-cyano-3-(pyridin-4-yl)-guanidine
Homo sapiens
2.4.2.12
N-(4-[[4-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
Homo sapiens
2.4.2.12
N-(pyridin-4-yl)cyclopropanecarboxamide
-
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-[(6-methylpyridin-3-yl)sulfonyl]benzyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
Homo sapiens
2.4.2.12
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
Homo sapiens
2.4.2.12
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
-
Homo sapiens
2.4.2.12
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
-
Homo sapiens
2.4.2.12
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
potent inhibitor
Homo sapiens
2.4.2.12
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
Homo sapiens
-
nicotinamide D-ribonucleotide + diphosphate
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.4.2.12
Homo sapiens
P43490
-
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
2.4.2.12
A-2780 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
MiaPaCa2 cell
-
Homo sapiens
-
2.4.2.12
PC-3 cell
-
Homo sapiens
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
736612
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.4.2.12
0.000001
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000011
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000003
-
pH and temperature not specified in the publication
Homo sapiens
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
2.4.2.12
0.0000038
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000044
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000047
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000051
-
pH and temperature not specified in the publication
Homo sapiens
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000066
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.0000072
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000076
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0000078
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0000088
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000009
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000095
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.000012
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000012
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000021
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.000036
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.000049
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
2.4.2.12
0.000062
-
pH and temperature not specified in the publication
Homo sapiens
1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
2.4.2.12
0.000063
-
pH and temperature not specified in the publication
Homo sapiens
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
2.4.2.12
0.00046
-
pH and temperature not specified in the publication
Homo sapiens
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0013
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
2.4.2.12
0.0015
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0016
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
N-(pyridin-4-yl)cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
2.4.2.12
0.23
-
pH and temperature not specified in the publication
Homo sapiens
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.4.2.12
0.000001
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000011
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000003
-
pH and temperature not specified in the publication
Homo sapiens
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
2.4.2.12
0.0000038
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000044
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000047
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000051
-
pH and temperature not specified in the publication
Homo sapiens
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000066
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.0000072
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000076
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0000078
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0000088
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000009
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0000095
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.000012
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000012
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.000021
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.000036
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
2.4.2.12
0.000049
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
2.4.2.12
0.000062
-
pH and temperature not specified in the publication
Homo sapiens
1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
2.4.2.12
0.000063
-
pH and temperature not specified in the publication
Homo sapiens
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
2.4.2.12
0.00046
-
pH and temperature not specified in the publication
Homo sapiens
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
2.4.2.12
0.0013
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
2.4.2.12
0.0015
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
2.4.2.12
0.0016
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
N-(pyridin-4-yl)cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
2.4.2.12
0.002
-
pH and temperature not specified in the publication
Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
2.4.2.12
0.23
-
pH and temperature not specified in the publication
Homo sapiens
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.4.2.12
1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
Homo sapiens
2.4.2.12
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
-
Homo sapiens
2.4.2.12
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
-
Homo sapiens
2.4.2.12
FK866
i.e. (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
2.4.2.12
GMX-1778
i.e. (E)-1-(6-(4-chlorophenoxy)hexyl)-2-cyano-3-(pyridin-4-yl)-guanidine
Homo sapiens
2.4.2.12
N-(4-[[4-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
Homo sapiens
2.4.2.12
N-(pyridin-4-yl)cyclopropanecarboxamide
-
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-[(6-methylpyridin-3-yl)sulfonyl]benzyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
Homo sapiens
2.4.2.12
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
Homo sapiens
2.4.2.12
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
-
Homo sapiens
2.4.2.12
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
-
Homo sapiens
2.4.2.12
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
potent inhibitor
Homo sapiens
2.4.2.12
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
Homo sapiens
2.4.2.12
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
Homo sapiens
-
nicotinamide D-ribonucleotide + diphosphate
-
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
2.4.2.12
A-2780 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
MiaPaCa2 cell
-
Homo sapiens
-
2.4.2.12
PC-3 cell
-
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.4.2.12
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
736612
Homo sapiens
nicotinamide D-ribonucleotide + diphosphate
-
-
-
?