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2-hydroxyphenylethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
i.e. o-octopamine
-
-
?
3,4-dichlorophenyl ethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
3,4-dichlorophenylethanolamine + S-adenosyl-L-methionine
N-methyl-3,4-dichlorophenylethanolamine + S-adenosyl-L-homocysteine
3,4-dichlorophenylethylenediamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
3,4-dihydroxynorephedrine + S-adenosyl-L-methionine
3,4-dihydroxyephedrine + S-adenosyl-L-homocysteine
-
18% of the activity with normetanephrine
-
-
?
3-chloro-4-hydroxyphenylethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
3-hydroxyphenylethanolamine + S-adenosyl-L-methionine
N-methyl-m-octopamine + S-adenosyl-L-homocysteine
3-trifluoromethylphenylethanolamine + S-adenosyl-L-methionine
?
-
-
-
?
3-trifluoromethylphenylethanolamine + S-adenosyl-L-methionine
N-methyl-3-trifluoromethylphenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
?
4-hydroxynorephedrine + S-adenosyl-L-methionine
4-hydroxyephedrine + S-adenosyl-L-homocysteine
-
18% of the activity with normetanephrine
-
-
?
4-hydroxyphenylethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
i.e. octopamine
-
-
?
9-methylnorharman + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
anti-9-amino-6-(trifluoromethyl)benzonorbornene + S-adenosyl-L-methionine
?
-
-
-
?
cis-(1R,2S)-2-amino-1-tetralol + S-adenosyl-L-methionine
cis-(1R,2S)-2-methylamino-1-tetralol + S-adenosyl-L-homocysteine
-
-
-
?
D-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
DL-m-hydroxyphenylethanolamine + S-adenosyl-L-methionine
neosynephrine + S-adenosyl-L-homocysteine
-
60% of the activity with normetanephrine
-
-
?
DL-neo-synephrine + S-adenosyl-L-methionine
3-hydroxy-alpha-[(dimethylamine)methyl]benzenemethanol + S-adenosyl-L-homocysteine
-
20% of the activity with normetanephrine
-
-
?
DL-octopamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
18% of the activity with normetanephrine
-
-
?
dopamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
epinephrine + S-adenosyl-L-methionine
? + D-adenosylhomocysteine
-
-
-
-
?
L-norephedrine + S-adenosyl-L-methionine
ephedrine + S-adenosyl-L-homocysteine
-
14% of the activity with normetanephrine
-
-
?
L-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
normetanephrine + S-adenosyl-L-methionine
metanephrine + S-adenosyl-L-homocysteine
octopamine + S-adenosyl-L-methionine
N-methyloctopamine + S-adenosyl-L-homocysteine
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
S-adenosyl-L-methionine + 4-aminomethyl-1,2,3,4-tetrahydroisoquinoline
S-adenosyl-L-homocysteine + ?
-
-
-
?
S-adenosyl-L-methionine + noradrenaline
S-adenosyl-L-homocysteine + epinephrine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
S-adenosyl-L-methionine + phenylethanolamine
S-adenosyl-L-homocysteine + N-methylphenylethanolamine
additional information
?
-
3,4-dichlorophenylethanolamine + S-adenosyl-L-methionine
N-methyl-3,4-dichlorophenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
-
?
3,4-dichlorophenylethanolamine + S-adenosyl-L-methionine
N-methyl-3,4-dichlorophenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
-
?
3,4-dichlorophenylethylenediamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
3,4-dichlorophenylethylenediamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
3-chloro-4-hydroxyphenylethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
3-chloro-4-hydroxyphenylethanolamine + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
-
-
-
?
3-hydroxyphenylethanolamine + S-adenosyl-L-methionine
N-methyl-m-octopamine + S-adenosyl-L-homocysteine
-
-
-
?
3-hydroxyphenylethanolamine + S-adenosyl-L-methionine
N-methyl-m-octopamine + S-adenosyl-L-homocysteine
-
i.e. m-octopamine
-
-
?
9-methylnorharman + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
2N-methylation
-
-
?
9-methylnorharman + S-adenosyl-L-methionine
? + S-adenosyl-L-homocysteine
-
PNMT catalyzes the 2N-methylation of beta-carbolines, forming 2N-methylated beta-carbolinium cations, which are structural and functional analogs of the Parkinsonian-inducing toxin MPP+
-
-
?
D-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
15% of the activity with normetanephrine
-
-
?
D-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
L-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
L-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
21% of the activity with normetanephrine
-
-
?
L-norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
?
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
?
norepinephrine + S-adenosyl-L-methionine
epinephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
normetanephrine + S-adenosyl-L-methionine
metanephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
normetanephrine + S-adenosyl-L-methionine
metanephrine + S-adenosyl-L-homocysteine
-
-
-
-
?
normetanephrine + S-adenosyl-L-methionine
metanephrine + S-adenosyl-L-homocysteine
-
i.e. 3-methoxy-4-hydroxyphenylethanolamine
-
-
?
octopamine + S-adenosyl-L-methionine
N-methyloctopamine + S-adenosyl-L-homocysteine
-
-
-
?
octopamine + S-adenosyl-L-methionine
N-methyloctopamine + S-adenosyl-L-homocysteine
-
-
-
-
?
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
-
?
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
?
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
-
?
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
-
72% of the activity with normetanephrine
-
-
?
phenylethanolamine + S-adenosyl-L-methionine
N-methylphenylethanolamine + S-adenosyl-L-homocysteine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
last step in biosynthesis of epinephrine
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
terminal step in epinephrine biosynthesis
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
epinephrine is an important neurotransmitter and hormone, and epinephrine is required for normal blood pressure and cardiac filling responses to stress, but is not required for tachycardia during stress or normal cardiovascular function at rest
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
epinephrine is an important neurotransmitter and hormone, and epinephrine is required for normal blood pressure and cardiac filling responses to stress, but is not required for tachycardia during stress or normal cardiovascular function at rest
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
-
-
-
?
S-adenosyl-L-methionine + norepinephrine
S-adenosyl-L-homocysteine + epinephrine
-
last step in biosynthesis of epinephrine
-
-
?
S-adenosyl-L-methionine + phenylethanolamine
S-adenosyl-L-homocysteine + N-methylphenylethanolamine
-
-
-
-
?
S-adenosyl-L-methionine + phenylethanolamine
S-adenosyl-L-homocysteine + N-methylphenylethanolamine
-
-
-
?
S-adenosyl-L-methionine + phenylethanolamine
S-adenosyl-L-homocysteine + N-methylphenylethanolamine
-
-
-
-
?
additional information
?
-
-
enzyme is involved in biosynthesis of epinephrine
-
-
?
additional information
?
-
-
the enzyme is involved in norepinephrine pathways
-
-
?
additional information
?
-
-
enzyme does not react with benzylisoquinolines: tetrahydropapaveroline (THP), 6-O-methyl-THP, 4'-O-methyl-THP and norreticuline
-
-
?
additional information
?
-
enzyme operates by an ordered sequential mechanism in which AdoMet binds first. A protonated and an unprotonated group are required for catalysis
-
-
?
additional information
?
-
-
enzyme operates by an ordered sequential mechanism in which AdoMet binds first. A protonated and an unprotonated group are required for catalysis
-
-
?
additional information
?
-
-
the phenylethanolamine N-methyltransferase GRE plays a necessary, but not sufficient role in the transcriptional aspects to the control mechanism. Analyses implicate the participation of sequences in the distal 5´promoter of this gene.
-
-
?
additional information
?
-
-
terminal enzyme in the biosynthetic pathway for epinephrine
-
-
?
additional information
?
-
-
terminal enzyme in epinephrine biosynthesis
-
-
?
additional information
?
-
-
final enzyme in the pathway for epinephrine biosynthesis
-
-
?
additional information
?
-
-
the enzyme binds to the alpha-adrenoreceptor
-
-
?
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(6R)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
(6R)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
(6S)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
(6S)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
(7-nitro-1,2,3,4-tetrahydroisoquinolin-3-yl)methanol
-
-
(R)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
(R)-7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
-
(S)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
1,2,3,4-tetrahydrobenz[h]isoquinoline
1,2,3,4-tetrahydroisoquinoline
1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid
-
-
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
1,4-diaminonaphthalene-2,6-disulfonic acid
-
-
1-(2,3-dichlorophenyl)ethanamine
-
-
1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)ethanone
-
-
1-aminoisoquinoline
-
Kd: 14 microM
1-thiophen-2-ylmethanamine
-
-
1-thiophen-3-ylmethanamine
-
-
2,3,4,5-tetrahydro-1H-2-benzazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzodiazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzothiazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzoxazepine
-
-
2,3-dichloro-alpha-methylbenzylamine
-
2,5-Dimethyl-1-aminobenzimidazole
2-amino-1-methylbenzimidazole
-
Kd: 4.6 microM
2-amino-4(7)-hydroxy-benzimidazole
-
Kd: 20 microM
2-amino-5(6)-chloro-7(4)-hydroxy-benzimidazole
-
Kd: 14 microM
2-amino-5(6)-chloro-benzimidazole
-
Kd: 1.8 microM
2-amino-5(6)-fluoro-benzimidazole
-
Kd: 7.2 microM
2-aminobenzimidazole
-
Kd: 6.3 microM
2-Aminotetralin
-
most effective inhibitor
2-bromo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-chlorophenylethanolamine
-
-
2-fluorophenylethanolamine
-
-
2-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-thiophen-2-ylethanamine
-
-
3,4-Dichlorophenylethanolamine
3,4-dichlorophenylethylenediamine
-
substrate inhibition
3,4-dihydroxyphenylethanolamine
-
-
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
very high selectivity
3-(fluoromethyl)-7-(thiomorpholin-4-ylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-(fluoromethyl)-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-(fluoromethyl)-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
very high selectivity
3-(fluoromethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
3-(trifluoromethyl)-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
-
3-bromophenylethanolamine
-
-
3-butyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(ethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-2,2,2-trifluoroethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-3-methoxypropylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-4-nitrophenylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(propylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-ethyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-ethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-ethyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-fluoromethyl-7-(2,2,2-trifluoroethylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(3,3,3-trifluoropropylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(4,4,4-trifluorobutylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(4-chlorobenzylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(N-benzylaminosulfonyl)-1,2,3,4-tetrahydrosioquinoline
-
-
3-fluoromethyl-7-(N-methylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-azido-1,2,3,4-tetrahydrosioquinoline
-
-
3-fluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
3-fluoromethyl-7-isothiocyanato-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-methanesulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-propylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-[N-(4-chlorophenyl)aminosulfonyl]-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-hydroxymethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-hydroxypropyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
extension of the 3-hydroxyalkyl chain by just one carbon results in a significant loss in phenylethanolamine N-methyltransferse inhibitory potency
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-isopropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-methyl-1,2,3,4-tetrahydroisoquinoline
3-methyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-methyl-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
-
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-methyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-propyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-propyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-thienylmethylamine
-
inhibits the enzyme and is selective toward the alpha2-adrenoceptor
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines
-
several 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines and some enantiomers of 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines. For the phenylethanolamine N-methyltransferase inhibitory potency of different 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines, compounds bearing a lipophilic 7-substituent show higher potency than compounds bearing a hydrophilic 7-substituent. Comparison to the inhibitory activity of the entantiomers of the most potent racemates show that the R-enantiomers are approximately 4fold as potent as their corresponding S-enantiomers.
-
3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
-
4-(benzo[d][1,3]dioxol-5-ylamino)-4-oxobutanoic acid
-
-
4-bromo-1H-imidazole
-
Kd: 170 microM
4-bromophenylethanolamine
-
-
4-fluorophenylethanolamine
-
-
4-hydroxyphenylethanolamine
-
-
4-oxo-1,4-dihydroquinoline-3,7-dicarboxylic acid
-
-
4-quinolinol
-
Kd: 690 microM
5,6-Dichloro-2-aminotetralin
-
0.00093 mM, 50% inhibition, competitive with norepinephrine as substrate
5-chlorobenzimidazole
-
Kd: 97 microM
6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-Aminoquinoline
-
Kd: 380 microM
6-Chloropurine
-
Kd: 140 microM
6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
7-(3-methoxypropylsulfonyl)-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-(N-4-chlorophenylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-(N-butylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-acetamido-1,2,3,4-tetrahydroisoquinoline
-
-
7-allylsulfonyl-1,2,3,4-tetrahydrosioquinoline
-
-
7-aminocarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-aminomethyl-1,2,3,4-tetrahydroisoquinoline dihydrochloride
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline
-
i.e. SK&F 29661
7-aminosulfonyl-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-benzoyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-benzyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenzo[h]isoquinoline
-
7-bromo-1,2,3,4-tetrahydroben[h]isoquinoline is 2fold more potent as an inhibitor of phenylethanolamine N-methyltransferase than 1,2,3,4-tetrahydroben[h]isoquinoline.
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-bromo-1,2,3,4-tetrahydroisoquinoline
7-bromo-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
7-bromo-3-butyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-ethyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-hydroxyethyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-3-hydroxypropyl-1,2,3,4-tetrahydroisoquinoline
-
little selcetivity
7-bromo-3-isopropyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
7-bromo-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-N-triphenylmethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-butylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-ethylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline oxalate
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfinyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfonyl-3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylthio-1,2,3,4-tetrahydroisoquinoline
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-nitro-1,2,3,4-tetrahydroisoquinoline
7-nitro-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-nitro-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
7-trichloromethylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
D-norepinephrine
-
substrate inhibition
dopamine
-
competitive inhibition with respect to phenylethanolamine
human cerebrospinal fluid
-
-
-
L-norepinephrine
-
substrate inhibition
methanol
-
at nonsaturating concentrations of phenylethanolamine, methanol inhibits in a competitive fashion. With respect to S-adenosyl-L-methionine inhibition by methanol is noncompetitive
N-(4-chlorophenyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
N-(4-chlorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
octopamine
-
at high concentrations
p-hydroxymercuribenzoate
-
0.00001 mM, 75% loss of activity
phenylethanolamine
-
at high concentrations
Phenylethylamine
-
competitive inhibition with respect to phenylethanolamine
R-(+)-7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
-
SKF 64139
1,2,3,4-tetrahydroisoquinoline derivate with two chloro substituents on the aromatic ring. Is able to cross the blood-brain barrier.
trans-(1S,2S)-2-amino-1-tetralol
-
tyramine
-
at high concentrations
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
the inhibitor forms hydrophobic interactions with Val53, Met258, Val272, and Val269 in the PNMT active site, binding site structure, overview
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
the inhibitor forms hydrophobic interactions with Val53, Met258, Val272, and Val269 in the PNMT active site, binding site structure, overview
1,2,3,4-tetrahydroisoquinoline
-
a nonselective inhibitor
1,2,3,4-tetrahydroisoquinoline
-
-
1,2,3,4-tetrahydroisoquinoline
-
a nonselective inhibitor
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
2,5-Dimethyl-1-aminobenzimidazole
-
-
2,5-Dimethyl-1-aminobenzimidazole
-
-
3,4-dichloroamphetamine
-
3,4-dichloroamphetamine
-
-
3,4-Dichlorophenylethanolamine
-
substrate inhibition
3,4-Dichlorophenylethanolamine
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
extension of the 3-hydroxyalkyl chain by just one carbon results in a significant loss in phenylethanolamine N-methyltransferse inhibitory potency
3-methyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
i.e. SK&F 64139
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
i.e. LY 134046
epinephrine
-
-
epinephrine
-
noncompetitive with normetanephrine as substrate
epinephrine
-
isoenzyme E2, noncompetitive inhibitor of S-adenosyl-L-methionine
LY134046
-
selective inhibitor, IC50: 0.0019 mM
LY134046
2,3,4,5-tetrahydro-1H-2-benzyzepine derivate with two chloro substituents on the aromatic ring. Is able to cross the blood-brain barrier.
norepinephrine
-
noncompetitive inhibition with phenylethanolamine as substrate, competitive inhibition with normetanephrine as substrate
norepinephrine
-
4 distinct substrate inhibition patterns: enzyme form E1 is not subject to substrate inhibition, isoenzyme E-2 is inhibited by S-adenosyl-L-methionine and norepinephrine, isoenzyme E-3 and E-4 are inhibited by norepinephrine only, isoenzyme E5 is inhibited only by S-adenosyl-L-methionine
norepinephrine
-
at high concentrations
PCMB
-
-
PCMB
-
0.01 mM, complete inhibition
S-adenosyl-L-methionine
-
substrate inhibition
S-adenosyl-L-methionine
-
4 distinct substrate inhibition patterns: enzyme form E1 is not subject to substrate inhibition, isoenzyme E-2 is inhibited by S-adenosyl-L-methionine and norepinephrine, isoenzyme E-3 and E-4 are inhibited by norepinephrine only, isoenzyme E5 is inhibited only by S-adenosyl-L-methionine
S-adenosylhomocysteine
-
competitive
S-adenosylhomocysteine
-
-
SKF 29661
1,2,3,4-tetrahydroisoquinoline derivate
additional information
-
7-substituted-1,2,3,4-tetrahydroisoquinolines are potent inhibitors, unfortunately, most of these compounds also exhibit a strong affinity for the alpha2-adrenoreceptor
-
additional information
-
inhibitor docking studies, molecular modelling; the addition of a 7-substituent (NO2, SO2NH2, OMe, OH, or CN) to 1,2,3,4-tetrahydroben[h]isoquinoline does not lead to an increase in phenylethanolamine N-methyltransferase inhibitory potency.
-
additional information
-
the rank order of phenylethanolamine N-methyltransferase inhibitory potency for the analysed 3,7-disubstituted-1,2,3,4-tetrahydroisoquinoline is CH2F equal to CHF2 decreases to CF3. The 3-difluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines have the proper balance of steric and pKa properties, they are both potent inhibitors of phenylethanolamine N-methyltransferase and highly selective due to low affinity for the alpha2-adrenoceptor.
-
additional information
the series of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines is more lipophilic but less potent than the correspnding sulfonamides. The interaction of the human phenylethanolamnie N-methyltransferase main chain carbonyl oxygen of Asn39 with the sulfonamide -NH- is likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfones.
-
additional information
-
the series of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines is more lipophilic but less potent than the correspnding sulfonamides. The interaction of the human phenylethanolamnie N-methyltransferase main chain carbonyl oxygen of Asn39 with the sulfonamide -NH- is likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfones.
-
additional information
-
importance of protein flexibility in structure-based inhibitor design
-
additional information
-
inhibitor docking studies, molecular modelling
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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0.676
2-hydroxyphenylethanolamine
-
-
0.0008 - 0.00159
3,4-Dichlorophenylethanolamine
0.012 - 0.0131
3,4-dichlorophenylethylenediamine
0.013
3,4-dihydroxyphenylethanolamine
-
-
0.0024
3-chloro-4-hydroxyphenylethanolamine
-
-
0.089
3-hydroxyphenylethanolamine
-
-
0.366
3-methoxy-4-hydroxy-phenylethanolamine
-
-
0.00054 - 0.055
3-trifluoromethylphenylethanolamine
0.047
4-aminomethyl-1,2,3,4-tetrahydroisoquinoline
-
0.017
4-hydroxyphenylethanolamine
-
-
0.0015 - 0.025
anti-9-amino-6-(trifluoromethyl)benzonorbornene
0.0053
cis-(1R,2S)-2-amino-1-tetralol
wild type enzyme, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.0297 - 0.109
D-norepinephrine
0.015 - 0.101
L-norepinephrine
0.0184
norepinephrine
-
wild-type enzyme
0.07 - 2.05
phenylethanolamine
0.0012 - 0.045
S-adenosyl-L-methionine
additional information
additional information
-
Km-value of mutant enzymes
-
0.0008
3,4-Dichlorophenylethanolamine
-
-
0.00132
3,4-Dichlorophenylethanolamine
-
enzyme form H-2
0.00159
3,4-Dichlorophenylethanolamine
-
enzyme form H-1
0.012
3,4-dichlorophenylethylenediamine
-
enzyme form H-2
0.0131
3,4-dichlorophenylethylenediamine
-
enzyme form H-1
0.00054
3-trifluoromethylphenylethanolamine
pH 8.0, 30°C
0.00055
3-trifluoromethylphenylethanolamine
wild type enzyme, assay containing S-adenosyl-L-methionine and 3-trifluoromethylphenylethanolamine
0.055
3-trifluoromethylphenylethanolamine
mutant D267, assay containing S-adenosyl-L-methionine and 3-trifluoromethylphenylethanolamine
0.0015
anti-9-amino-6-(trifluoromethyl)benzonorbornene
wild type enzyme, assay containing S-adenosyl-L-methionine and anti-9-amino-6-(trifluoromethyl)benzonorbornene
0.025
anti-9-amino-6-(trifluoromethyl)benzonorbornene
mutant D267A, assay containing S-adenosyl-L-methionine and anti-9-amino-6-(trifluoromethyl)benzonorbornene
0.0297
D-norepinephrine
-
enzyme form H-1
0.109
D-norepinephrine
-
enzyme form H-2
0.015
L-norepinephrine
-
-
0.0299
L-norepinephrine
-
enzyme form H-2
0.0428
L-norepinephrine
-
enzyme form H-1
0.101
L-norepinephrine
-
-
0.0055
octopamine
pH 8.0, 30°C
0.0055
octopamine
wild type enzyme, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.07
phenylethanolamine
-
0.077
phenylethanolamine
-
-
0.095
phenylethanolamine
-
purified in the absence of reducing agent, dimer, His-tagged
0.099
phenylethanolamine
wild type enzyme, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.1
phenylethanolamine
pH 8.0, 30°C
0.1
phenylethanolamine
wild type enzyme, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.101
phenylethanolamine
mutant E185Q, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.102
phenylethanolamine
mutant E185A, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.179
phenylethanolamine
mutant E219Q, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.226
phenylethanolamine
-
enzyme form H-2
0.244
phenylethanolamine
-
enzyme form H-1
0.32
phenylethanolamine
mutant E185D, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.58
phenylethanolamine
mutant E219A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
1.31
phenylethanolamine
mutant K57A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
1.63
phenylethanolamine
mutant V53A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
1.64
phenylethanolamine
mutant D267N, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
1.73
phenylethanolamine
mutant Y35F, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
2.05
phenylethanolamine
mutant D267A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.0012
S-adenosyl-L-methionine
wild type enzyme, assay containing S-adenosyl-L-methionine and 3-trifluoromethylphenylethanolamine
0.0012
S-adenosyl-L-methionine
cosubstrate 3-trifluoromethylphenylethanolamine, pH 8.0, 30°C
0.0013
S-adenosyl-L-methionine
mutant E185Q, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.0017
S-adenosyl-L-methionine
mutant E185A, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.002
S-adenosyl-L-methionine
wild type enzyme, assay containing S-adenosyl-L-methionine and anti-9-amino-6-(trifuoromethyl)benzonorbornene
0.0024
S-adenosyl-L-methionine
mutant D267, assay containing S-adenosyl-L-methionine and 3-trifluoromethylphenylethanolamine
0.0034
S-adenosyl-L-methionine
wild type enzyme, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.0034
S-adenosyl-L-methionine
wild type enzyme, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.0034
S-adenosyl-L-methionine
cosubstrate phenylethanolamine, pH 8.0, 30°C
0.0035
S-adenosyl-L-methionine
-
purified in the absence of reducing agent, dimer, His-tagged
0.0051
S-adenosyl-L-methionine
mutant D267A, assay containing S-adenosyl-L-methionine and anti-9-amino-6-(trifluoromethyl)benzonorbornene
0.00543
S-adenosyl-L-methionine
-
enzyme form H-1
0.0067
S-adenosyl-L-methionine
mutant E219Q, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.0067
S-adenosyl-L-methionine
cosubstrate octopamine, pH 8.0, 30°C
0.0071
S-adenosyl-L-methionine
mutant E219A and mutant D267N, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.0081
S-adenosyl-L-methionine
mutant D267A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.0096
S-adenosyl-L-methionine
mutant V53A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.0117
S-adenosyl-L-methionine
mutant K57A, radiochemical assay containing S-adenosyl-L-methionine and phenylethanolamine
0.014
S-adenosyl-L-methionine
mutant E185D, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
0.0149
S-adenosyl-L-methionine
-
enzyme form H-2
0.0194
S-adenosyl-L-methionine
-
wild-type enzyme
0.024
S-adenosyl-L-methionine
-
-
0.045
S-adenosyl-L-methionine
mutant Y35F, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C.
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0.0096
(6R)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
R-isomer, pH 8.0, 37°C
0.15
(6R)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
R-isomer, pH 8.0, 37°C
0.00031
(6S)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
S-isomer, pH 8.0, 37°C
0.0033
(6S)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
S-isomer, pH 8.0, 37°C
0.000017 - 0.000145
(7-nitro-1,2,3,4-tetrahydroisoquinolin-3-yl)methanol
0.0383
(R)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00101
(S)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00049
1,2,3,4-tetrahydrobenz[h]isoquinoline
0.0058
1,2,3,4-tetrahydroisoquinoline
0.47
1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid
-
-
0.00012 - 0.0069
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
0.00009
1-(2,3-dichlorophenyl)ethanamine
-
pH 8.0
0.061
1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)ethanone
-
pH 8.0, 37°C
0.45
1-thiophen-2-ylmethanamine
-
pH 8.0, 37°C
0.11
1-thiophen-3-ylmethanamine
-
pH 8.0, 37°C
0.00334
2,3,4,5-tetrahydro-1H-2-benzazepine
-
-
0.028
2,3,4,5-tetrahydro-5H-1,4-benzodiazepine
-
-
0.0041
2,3,4,5-tetrahydro-5H-1,4-benzothiazepine
-
-
0.0212
2,3,4,5-tetrahydro-5H-1,4-benzoxazepine
-
-
0.000072 - 0.00133
2,3-dichloro-alpha-methylbenzylamine
0.0012
2-bromo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.00073 - 0.021
2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
0.025
2-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.0026
2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.22
2-Phenylethylamine
-
pH 8.0, 37°C
0.3
2-thiophen-2-ylethanamine
-
pH 8.0, 37°C
0.00227 - 0.0148
3,4-dichloroamphetamine
0.508 - 0.909
3,4-Dichlorophenylethanolamine
1.138 - 1.522
3,4-dichlorophenylethylenediamine
0.00082
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00015
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.0000018 - 0.000315
3-(fluoromethyl)-7-(thiomorpholin-4-ylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
0.00015
3-(fluoromethyl)-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00013
3-(fluoromethyl)-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.000017 - 0.000035
3-(fluoromethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
0.017
3-(trifluoromethyl)-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.0066
3-butyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.0034
3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0032
3-difluoromethyl-7-(ethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.00025
3-difluoromethyl-7-(N-2,2,2-trifluoroethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0053
3-difluoromethyl-7-(N-3-methoxypropylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.037
3-difluoromethyl-7-(N-4-nitrophenylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0021
3-difluoromethyl-7-(propylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.000094
3-difluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0031
3-difluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0002
3-difluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.006
3-difluoromethyl-7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.00017
3-difluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.000067
3-difluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0018
3-ethyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.00049
3-ethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00051
3-ethyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.0014
3-fluoromethyl-7-(2,2,2-trifluoroethylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.0013
3-fluoromethyl-7-(3,3,3-trifluoropropylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.067
3-fluoromethyl-7-(4,4,4-trifluorobutylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.032
3-fluoromethyl-7-(4-chlorobenzylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.0065
3-fluoromethyl-7-(N-benzylaminosulfonyl)-1,2,3,4-tetrahydrosioquinoline
-
-
0.0024
3-fluoromethyl-7-(N-methylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
0.00066
3-fluoromethyl-7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.0017
3-fluoromethyl-7-azido-1,2,3,4-tetrahydrosioquinoline
-
-
0.00064
3-fluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
0.0011
3-fluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
0.000073 - 0.00021
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
0.00057
3-fluoromethyl-7-isothiocyanato-1,2,3,4-tetrahydroisoquinoline
-
-
0.0016
3-fluoromethyl-7-methanesulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.54
3-fluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
0.0024
3-fluoromethyl-7-propylsulfonyl-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.00032
3-fluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00074
3-fluoromethyl-7-[N-(4-chlorophenyl)aminosulfonyl]-1,2,3,4-tetrahydroisoquinoline
-
-
0.00035
3-hydroxyethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
0.00051
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
0.000047
3-hydroxymethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0017
3-hydroxypropyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
0.0014
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
0.0046
3-isopropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.0014
3-methyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.000077
3-methyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.000067
3-methyl-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.000072
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.000034
3-methyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.00012
3-propyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.00092
3-propyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.015
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00052
3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
0.013
3-trifluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
0.002
3-trifluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
0.037
4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.015
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
pH 8.0, 37°C
0.1
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
pH 8.0, 37°C
0.00027
5,6-Dichloro-2-aminotetralin
-
-
0.04
6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.0058
6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.0000016 - 0.0000031
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
0.072
7-(3-methoxypropylsulfonyl)-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamnie as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.0009
7-(N-4-chlorophenylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0056
7-(N-butylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.19
7-acetamido-1,2,3,4-tetrahydroisoquinoline
-
-
0.0098
7-allylsulfonyl-1,2,3,4-tetrahydrosioquinoline
-
-
0.064
7-aminocarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
1.9
7-aminomethyl-1,2,3,4-tetrahydroisoquinoline dihydrochloride
-
-
0.033
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
0.00068
7-aminosulfonyl-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor
0.0029
7-benzoyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.061
7-benzyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00022
7-bromo-1,2,3,4-tetrahydrobenzo[h]isoquinoline
-
-
0.00022
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
0.000056
7-bromo-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.000023
7-bromo-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.0076
7-bromo-3-butyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00048
7-bromo-3-ethyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00035
7-bromo-3-hydroxyethyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.000012
7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0017
7-bromo-3-hydroxypropyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0044
7-bromo-3-isopropyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.000017
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.011
7-bromo-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00048
7-bromo-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00029
7-bromo-N-triphenylmethyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.018
7-butylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.0023
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
0.014
7-ethylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
inhibition constants are determine using four concentrations of phenylethanolamnie as the variable substrate and three concentrations of inhibitor with a radiochemical assay.
0.00091
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
0.011
7-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline oxalate
-
-
0.00004 - 0.00074
7-iodo-1,2,3,4-tetrahydroisoquinoline
0.0021
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
0.0067
7-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.045
7-methylsulfinyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.0013
7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.036
7-methylsulfonyl-3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00061
7-methylthio-1,2,3,4-tetrahydroisoquinoline
-
-
0.0009
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
0.00004 - 0.067
7-nitro-1,2,3,4-tetrahydroisoquinoline
0.0098
7-nitro-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00053
7-nitro-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.014
7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00028 - 0.00056
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
0.0013
7-trichloromethylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.0057
7-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.00018
7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
0.0000044 - 0.00026
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
0.17
benzylamine
-
pH 8.0, 37°C
0.109 - 8.298
D-norepinephrine
8
dopamine
-
competitive with phenylethanolamine
0.165 - 0.631
L-norepinephrine
0.0000044 - 0.00312
LY134046
0.0000013 - 0.00021
N-(4-chlorophenyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
0.000001 - 0.00027
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
0.0000014 - 0.000039
N-(4-chlorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
0.0059
norepinephrine
-
noncompetitive with phenylethanolamine
3.6
Phenylethylamine
-
competitive with phenylethanolamine
0.0000049
R-(+)-7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0124 - 0.0894
S-adenosyl-L-methionine
0.000057 - 0.321
SKF 29661
0.00000155 - 0.001375
SKF 64139
0.0021
trans-(1S,2S)-2-amino-1-tetralol
wild type enzyme, assay mixture consists of 25 microl of 0.5 M phosphate buffer (pH 8.0), 5 microl of [methyl-3H]S-adenosyl-L-methionine containing approximately 2.5 X 10 00000 dpm, varying amounts of phenylethanolamine and unlabeled S-adenosyl-L-methionine, 20 microl enzyme and water at 30°C. The concentration of S-adenosyl-L-methionine is fixed on 5 microM.
additional information
additional information
-
0.000017
(7-nitro-1,2,3,4-tetrahydroisoquinolin-3-yl)methanol
-
pH 8.0, 30°C, wild-type enzyme
0.000145
(7-nitro-1,2,3,4-tetrahydroisoquinolin-3-yl)methanol
-
pH 8.0, 30°C, mutant G57A
0.00049
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
pH 8.0, 37°C
0.00049
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
pH 7.7, 25°C
0.0058
1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.0058
1,2,3,4-tetrahydroisoquinoline
-
pH 7.7, 25°C
0.00012
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, wild-type enzyme
0.00028
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 37°C
0.0069
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, mutant G57A
0.000072
2,3-dichloro-alpha-methylbenzylamine
binding of the inhibitor to the wild type human phenylethanolamine N-methyltransferase S-adenosyl-L-methionine complex
0.000121
2,3-dichloro-alpha-methylbenzylamine
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00133
2,3-dichloro-alpha-methylbenzylamine
free wild type human phenylethanolamine N-methyltransferase
0.00073
2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.021
2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
pH 8.0, 37°C
0.00227
3,4-dichloroamphetamine
binding of the inhibitor to the wild type human phenylethanolamine N-methyltransferase S-adenosyl-L-methionine complex
0.00364
3,4-dichloroamphetamine
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.0148
3,4-dichloroamphetamine
free wild type human phenylethanolamine N-methyltransferase
0.508
3,4-Dichlorophenylethanolamine
-
enzyme form H-2, substrate inhibition
0.909
3,4-Dichlorophenylethanolamine
-
enzyme form H-1, substrate inhibition
1.138
3,4-dichlorophenylethylenediamine
-
enzyme form H-2, substrate inhibition
1.522
3,4-dichlorophenylethylenediamine
-
enzyme form H-1, substrate inhibition
0.0000018
3-(fluoromethyl)-7-(thiomorpholin-4-ylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, mutant G57A
0.000315
3-(fluoromethyl)-7-(thiomorpholin-4-ylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, wild-type enzyme
0.000017
3-(fluoromethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, mutant G57A
0.000035
3-(fluoromethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, wild-type enzyme
0.000073
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.00021
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
0.00051
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
0.00051
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0014
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
0.0014
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0000016
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
pH 8.0, 30°C
0.0000031
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.0000031
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00022
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
pH 8.0, 37°C
0.00022
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
pH 7.7, 25°C
0.00004
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, wild-type enzyme
0.00037
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
0.00037
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
0.00074
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, mutant G57A
0.00004
7-nitro-1,2,3,4-tetrahydroisoquinoline
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.000056
7-nitro-1,2,3,4-tetrahydroisoquinoline
binding of the inhibitor to the wild type human phenylethanolamine N-methyltransferase S-adenosyl-L-methionine complex
0.00007
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, wild-type enzyme
0.000078
7-nitro-1,2,3,4-tetrahydroisoquinoline
pH 8.0, 30°C
0.000078
7-nitro-1,2,3,4-tetrahydroisoquinoline
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00012
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 37°C
0.00013
7-nitro-1,2,3,4-tetrahydroisoquinoline
mutant V53A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00074
7-nitro-1,2,3,4-tetrahydroisoquinoline
mutant K57A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00137
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0, 30°C, mutant G57A
0.00236
7-nitro-1,2,3,4-tetrahydroisoquinoline
free wild type human phenylethanolamine N-methyltransferase
0.0179
7-nitro-1,2,3,4-tetrahydroisoquinoline
mutant E219A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.067
7-nitro-1,2,3,4-tetrahydroisoquinoline
mutant D267A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00028
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
pH 8.0
0.00056
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
0.0000044
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
pH 8.0, 30°C
0.000012
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
pH 8.0
0.00026
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
0.109
D-norepinephrine
-
enzyme form H-2, substrate inhibition
8.298
D-norepinephrine
-
enzyme form H-1, substrate inhibition
0.165
L-norepinephrine
-
enzyme form H-1, substrate inhibition
0.631
L-norepinephrine
-
enzyme form H-2, substrate inhibition
0.0000044
LY134046
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.0000225
LY134046
mutant V53A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.0000906
LY134046
mutant K57A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00059
LY134046
mutant D267A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00312
LY134046
mutant E219A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.0000013
N-(4-chlorophenyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, mutant G57A
0.00021
N-(4-chlorophenyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, wild-type enzyme
0.000001
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, mutant G57A
0.000046
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, wild-type enzyme
0.00027
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0
0.0000014
N-(4-chlorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, mutant G57A
0.000039
N-(4-chlorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
pH 8.0, 30°C, wild-type enzyme
0.0124
S-adenosyl-L-methionine
-
enzyme form H-2, substrate inhibition
0.0894
S-adenosyl-L-methionine
-
enzyme form H-1, substrate inhibition
0.000057
SKF 29661
binding of the inhibitor to the wild type human phenylethanolamine N-methyltransferase S-adenosyl-L-methionine complex
0.00012
SKF 29661
pH 8.0, 30°C
0.00012
SKF 29661
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00062
SKF 29661
mutant V53A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00284
SKF 29661
free wild type human phenylethanolamine N-methyltransferase
0.0069
SKF 29661
mutant D57A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.189
SKF 29661
mutant E219A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.321
SKF 29661
mutant D267A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.00000155
SKF 64139
wild type enzyme, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.000019
SKF 64139
mutant V53A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.0000265
SKF 64139
mutant K57A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.000999
SKF 64139
mutant D267A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
0.001375
SKF 64139
mutant E219A, inhibition assay containing a fixed concentration of S-adenosyl-L-methionine and variable concentrations of the inhibitor and phenylethanolamine
additional information
additional information
-
-
-
additional information
additional information
-
-
-
additional information
additional information
-
enzyme kinetics using competitive tight-binding inhibition routine
-
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16
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2008
Homo sapiens
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Epinephrine is required for normal cardiovascular responses to stress in the phenylethanolamine N-methyltransferase knockout mouse
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116
1024-1031
2007
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Association study between reward dependence temperament and a polymorphism in the phenylethanolamine N-methyltransferase gene in a Japanese female population
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49
503-507
2008
Homo sapiens
brenda
Gee, C.L.; Drinkwater, N.; Tyndall, J.D.; Grunewald, G.L.; Wu, Q.; McLeish, M.J.; Martin, J.L.
Enzyme adaptation to inhibitor binding: A cryptic binding site in phenylethanolamine N-methyltransferase
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50
6441
2007
Homo sapiens
-
brenda
Grobe, N.; Ren, X.; Kutchan, T.M.; Zenk, M.H.
An (R)-specific N-methyltransferase involved in human morphine biosynthesis
Arch. Biochem. Biophys.
506
42-47
2011
Homo sapiens
brenda
Drinkwater, N.; Vu, H.; Lovell, K.M.; Criscione, K.R.; Collins, B.M.; Prisinzano, T.E.; Poulsen, S.A.; McLeish, M.J.; Grunewald, G.L.; Martin, J.L.
Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors
Biochem. J.
431
51-61
2010
Homo sapiens
brenda
Hou, Q.Q.; Wang, J.H.; Gao, J.; Liu, Y.J.; Liu, C.B.
QM/MM studies on the catalytic mechanism of phenylethanolamine N-methyltransferase
Biochim. Biophys. Acta
1824
533-541
2012
Homo sapiens
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Kang, D.I.; Lee, J.Y.; Kim, W.; Jeong, K.W.; Shin, S.; Yang, J.; Park, E.; Chae, Y.K.; Kim, Y.
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Homo sapiens
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Homo sapiens
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