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Literature summary for 2.3.1.97 extracted from

  • Brand, S.; Cleghorn, L.A.; McElroy, S.P.; Robinson, D.A.; Smith, V.C.; Hallyburton, I.; Harrison, J.R.; Norcross, N.R.; Spinks, D.; Bayliss, T.; Norval, S.; Stojanovski, L.; Torrie, L.S.; Frearson, J.A.; Brenk, R.; Fairlamb, A.H.; Ferguson, M.A.; Read, K.D.; Wyatt, P.G.; Gilbert, I.H.
    Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors (2012), J. Med. Chem., 55, 140-152.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development the enzyme N-myristoyltransferase represents a promising drug target Trypanosoma brucei

Inhibitors

Inhibitors Comment Organism Structure
1-acetyl-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-indole-5-sulfonamide
-
Trypanosoma brucei
2,6-dichloro-4-(1,2,3,4-tetrahydroisoquinolin-5-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
2,6-dichloro-4-(2-piperazin-1-ylpyridin-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
-
Trypanosoma brucei
2,6-dichloro-4-(isoquinolin-5-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
2,6-dichloro-4-[6-(piperazin-1-yl)pyridin-3-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
2,6-dichloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
2-oxo-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
-
Trypanosoma brucei
3',5'-dichloro-4'-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]biphenyl-3-carboxamide
-
Trypanosoma brucei
3,5-dichloro-3'-[(4-methylpiperazin-1-yl)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
-
Trypanosoma brucei
3,5-dichloro-3'-[(diethylamino)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
-
Trypanosoma brucei
3,5-dichloro-4'-[(4-methylpiperazin-1-yl)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
-
Trypanosoma brucei
3,5-dichloro-4'-[(diethylamino)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
-
Trypanosoma brucei
3-cyano-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-(1H-pyrazol-1-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-bromo-2,6-dichloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
-
Trypanosoma brucei
4-bromo-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzamide
-
Trypanosoma brucei
4-bromo-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-bromo-N-(2-methylpropyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzamide
-
Trypanosoma brucei
4-bromo-N-methyl-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-bromo-N-[(1,3,5-trimethyl-1H-pyrazol-4-yl)methyl]benzenesulfonamide
-
Trypanosoma brucei
4-cyano-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-(1H-pyrazol-3-yl)benzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-(2-methylpyridin-3-yl)benzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-(pyridin-3-yl)benzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-phenylbenzenesulfonamide
-
Trypanosoma brucei
4-methoxy-2,3,6-trimethyl-N-[(1,3,5-trimethyl-1H-pyrazol-4-yl)methyl]benzenesulfonamide
-
Trypanosoma brucei
4-[(4-bromophenoxy)methyl]-1,3,5-trimethyl-1H-pyrazole
-
Trypanosoma brucei
4-[[(4-bromophenyl)sulfonyl]methyl]-1,3,5-trimethyl-1H-pyrazole
-
Trypanosoma brucei
6-(2-methyl-1,3-thiazol-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-(benzylamino)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-(morpholin-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-([2-[4-(propan-2-yl)piperazin-1-yl]ethyl]amino)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-chloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[(1H-indol-5-ylmethyl)amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[2-(4-methylpiperazin-1-yl)ethylamino]pyridine-3-sulfonic acid (1,3,5-trimethyl-1H-pyrazol-4-yl)amide
-
Trypanosoma brucei
6-[3-(piperazin-1-yl)piperidin-1-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[3-(piperazin-1-yl)pyrrolidin-1-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(1-methylpiperidin-4-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(1H-imidazol-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(4-benzylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(4-methylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(4-phenylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(morpholin-4-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(piperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[2-(piperidin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[3-(dimethylamino)propyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
6-[[4-[(dimethylamino)methyl]benzyl](methyl)amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
-
Trypanosoma brucei
DDD85646
-
Homo sapiens
DDD85646
-
Trypanosoma brucei
N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Trypanosoma brucei
N-(1-propyl-3,5-dimethyl-1H-pyrazol-4-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-(3,5-dimethyl-1-propyl-1H-pyrazol-4-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-(3,5-dimethyl-1H-pyrazol-4-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-(4-bromobenzyl)-1,3,5-trimethyl-1H-pyrazol-4-amine
-
Trypanosoma brucei
N-(4-bromophenyl)-1,3,5-trimethyl-1H-pyrazole-4-carboxamide
-
Trypanosoma brucei
N-(4-bromophenyl)-1,3,5-trimethyl-1H-pyrazole-4-sulfonamide
-
Trypanosoma brucei
N-(imidazo[1,2-a]pyridin-3-yl)-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-benzyl-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-[1,3-dimethyl-5-(morpholin-4-yl)-1H-pyrazol-4-yl]-4-methoxy-2,3,6-trimethylbenzenesulfonamide
-
Trypanosoma brucei
N-[4-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]phenyl]acetamide
-
Trypanosoma brucei
tert-butyl 4-[2-([5-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]pyridin-2-yl]amino)ethyl]piperazine-1-carboxylate
-
Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme NMT-1
-
Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
myristoyl-CoA + peptide CAP5.5 N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein Homo sapiens CoA + N-myristoyl-peptide CAP5.5
-
?
myristoyl-CoA + peptide CAP5.5 N-myristoylation of the synthetic peptide CAP5.5, derived from the N-terminus of the Trypanosoma brucei CAP5.5 protein Trypanosoma brucei CoA + N-myristoyl-peptide CAP5.5
-
?

Synonyms

Synonyms Comment Organism
N-myristoyltransferase
-
Homo sapiens
N-myristoyltransferase
-
Trypanosoma brucei
NMT
-
Trypanosoma brucei
NMT-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens
22
-
assay at room temperature Trypanosoma brucei

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens
7.4
-
assay at Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
pH 7.4, 22°C Trypanosoma brucei 2,6-dichloro-4-(2-piperazin-1-ylpyridin-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
0.000005
-
pH 7.4, 22°C Trypanosoma brucei 3,5-dichloro-3'-[(4-methylpiperazin-1-yl)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
0.00002
-
pH 7.4, 22°C Trypanosoma brucei 3,5-dichloro-3'-[(diethylamino)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
0.00003
-
pH 7.4, 22°C Trypanosoma brucei 6-[3-(piperazin-1-yl)piperidin-1-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.00003
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(1-methylpiperidin-4-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.000034
-
pH 7.4, 22°C Trypanosoma brucei 4-bromo-2,6-dichloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
0.00011
-
pH 7.4, 22°C Trypanosoma brucei 6-[3-(piperazin-1-yl)pyrrolidin-1-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.00011
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(4-methylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.00014
-
pH 7.4, 22°C Trypanosoma brucei 6-[2-(4-methylpiperazin-1-yl)ethylamino]pyridine-3-sulfonic acid (1,3,5-trimethyl-1H-pyrazol-4-yl)amide
0.00029
-
pH 7.4, 22°C Trypanosoma brucei 2,6-dichloro-4-[6-(piperazin-1-yl)pyridin-3-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.00033
-
pH 7.4, 22°C Trypanosoma brucei 6-[(1H-indol-5-ylmethyl)amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.00036
-
pH 7.4, 22°C Trypanosoma brucei 6-[[4-[(dimethylamino)methyl]benzyl](methyl)amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.0009
-
pH 7.4, 22°C Trypanosoma brucei 3',5'-dichloro-4'-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]biphenyl-3-carboxamide
0.001
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(4-phenylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.001
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(piperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.001
-
pH 7.4, 22°C Trypanosoma brucei 6-([2-[4-(propan-2-yl)piperazin-1-yl]ethyl]amino)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.001
-
pH 7.4, 22°C Trypanosoma brucei 2,6-dichloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.0012
-
pH 7.4, 22°C Trypanosoma brucei 3,5-dichloro-4'-[(4-methylpiperazin-1-yl)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
0.0013
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(1H-imidazol-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.0013
-
pH 7.4, 22°C Trypanosoma brucei 6-(benzylamino)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.0019
-
pH 7.4, 22°C Trypanosoma brucei 6-(morpholin-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.0021
-
pH 7.4, 22°C Trypanosoma brucei 6-[[3-(dimethylamino)propyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.0028
-
pH 7.4, 22°C Trypanosoma brucei N-[4-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]phenyl]acetamide
0.0033
-
pH 7.4, 22°C Trypanosoma brucei 2-oxo-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide
0.0043
-
pH 7.4, 22°C Trypanosoma brucei 2,6-dichloro-4-(1,2,3,4-tetrahydroisoquinolin-5-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.0048
-
pH 7.4, 22°C Trypanosoma brucei 4-(1H-pyrazol-1-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.0086
-
pH 7.4, 22°C Trypanosoma brucei 1-acetyl-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-indole-5-sulfonamide
0.01
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(4-benzylpiperazin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.01
-
pH 7.4, 22°C Trypanosoma brucei tert-butyl 4-[2-([5-[(1,3,5-trimethyl-1H-pyrazol-4-yl)sulfamoyl]pyridin-2-yl]amino)ethyl]piperazine-1-carboxylate
0.011
-
pH 7.4, 22°C Trypanosoma brucei 3,5-dichloro-4'-[(diethylamino)methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)biphenyl-4-sulfonamide
0.012
-
pH 7.4, 22°C Trypanosoma brucei 6-(2-methyl-1,3-thiazol-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.012
-
pH 7.4, 22°C Trypanosoma brucei N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.014
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(piperidin-1-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.026
-
pH 7.4, 22°C Trypanosoma brucei 6-chloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.028
-
pH 7.4, 22°C Trypanosoma brucei 3-cyano-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.032
-
pH 7.4, 22°C Trypanosoma brucei 4-cyano-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.038
-
pH 7.4, 22°C Trypanosoma brucei 6-[[2-(morpholin-4-yl)ethyl]amino]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridine-3-sulfonamide
0.042
-
pH 7.4, 22°C Trypanosoma brucei 4-[[(4-bromophenyl)sulfonyl]methyl]-1,3,5-trimethyl-1H-pyrazole
0.049
-
pH 7.4, 22°C Trypanosoma brucei 2,6-dichloro-4-(isoquinolin-5-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
0.1
-
above, pH 7.4, 22°C Trypanosoma brucei N-(4-bromophenyl)-1,3,5-trimethyl-1H-pyrazole-4-sulfonamide
0.1
-
above, pH 7.4, 22°C Trypanosoma brucei N-(4-bromobenzyl)-1,3,5-trimethyl-1H-pyrazol-4-amine
0.1
-
above, pH 7.4, 22°C Trypanosoma brucei 4-[(4-bromophenoxy)methyl]-1,3,5-trimethyl-1H-pyrazole
0.1
-
above, pH 7.4, 22°C Trypanosoma brucei 4-bromo-N-[(1,3,5-trimethyl-1H-pyrazol-4-yl)methyl]benzenesulfonamide
0.1
-
above, pH 7.4, 22°C Trypanosoma brucei N-(4-bromophenyl)-1,3,5-trimethyl-1H-pyrazole-4-carboxamide