Any feedback?
Please rate this page
(all_enzymes.php)
(0/150)

BRENDA support

2.1.1.8: histamine N-methyltransferase

This is an abbreviated version!
For detailed information about histamine N-methyltransferase, go to the full flat file.

Word Map on EC 2.1.1.8

Reaction

S-adenosyl-L-methionine
+
histamine
=
S-adenosyl-L-homocysteine
 +
Ntau-methylhistamine

Synonyms

histamine 1-methyltransferase, histamine methyltransferase, histamine N-methyltransferase, histamine-methylating enzyme, histamine-N-methyltransferase, HMT, HNMT, imidazole methyltransferase, imidazole N-methyltransferase, imidazolemethyltransferase, methyltransferase, histamine, Ntau-methyltransferase, S-adenosylmethionine-histamine N-methyltransferase

ECTree

     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.1 Methyltransferases
                2.1.1.8 histamine N-methyltransferase

Inhibitors

Inhibitors on EC 2.1.1.8 - histamine N-methyltransferase

Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(5'-amino-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-yl)-[4-(3-piperidin-1-yl-propoxy)-phenyl]-methanone
-
50% inhibition at 0.0020 mM, simultaneously a highly potent H3 receptor ligand
(5'-nitro-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-yl)-[4-(3-piperidin-1-yl-propoxy)-phenyl]-methanone
-
50% inhibition at 0.0015 mM, simultaneously a highly potent H3 receptor ligand
(5-nitro-pyridin-2-yl)-[4-(3-piperidin-1-yl-propoxy)-benzyl]-amine
-
50% inhibition at 0.0042 mM, simultaneously a highly potent H3 receptor ligand
(5-nitro-pyridin-2-yl)-{2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-ethyl}-amine
-
50% inhibition at 0.0028 mM, simultaneously a highly potent H3 receptor ligand
(5-nitro-pyridin-2-yl)-{3-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propyl}-amine
-
50% inhibition at 0.0017 mM, simultaneously a highly potent H3 receptor ligand
(5-nitro-pyridin-2-yl)-{4-[4-(3-piperidin-1-yl-propoxy)-phenyl]-butyl}-amine
-
50% inhibition at 0.0017 mM, simultaneously a highly potent H3 receptor ligand
(R)-chloroquine
-
50% inhibition at 0.018 mM, liver enzyme, 50% inhibition at 0.0022 mM, brain enzyme
(S)-chloroquine
-
50% inhibition at 0.005 mM, liver enzyme, 50% inhibition at 0.007 mM, brain enzyme
1-(3-(4-(3,4-dihydro-2H-pyrrol-5-yl)phenoxy)propyl)piperidine
-
50% inhibition at 0.0090 mM, simultaneously a highly potent H3 receptor ligand
1-Methylhistamine
2-(3-piperidin-1-ylpropoxy)-1,3-benzothiazole quinoline
-
50% inhibition at 0.021 mM, simultaneously a highly potent H3 receptor ligand
-
2-(4-hydroperoxyphenyl)-6-methyl-4H-chromen-4-one
-
-
2-Bromolysergic acid diethylamide
-
-
2-Methylhistamine
-
strong
3,6-dimethyl-2-phenyl-4H-chromen-4-one
-
-
3-bromo-6-chloro-2-phenyl-4H-chromen-4-one
-
-
3-bromo-6-methyl-2-phenyl-4H-chromen-4-one
-
-
3-chloro-6-methyl-2-phenyl-4H-chromen-4-one
-
-
3-Methylhistamine
-
strong
4-(dimethylamino)butyl carbamimidothioate
-
SKF-91488
5-Methylhistamine
-
weak
5-nitro-2-(3-piperidin-1-ylpropoxy)pyridine
-
50% inhibition at 0.034 mM, simultaneously a highly potent H3 receptor ligand
5-nitro-N-(4-(3-piperidin-1-ylpropoxy)phenyl)pyridin-2-amine
-
50% inhibition at 0.0038 mM, simultaneously a highly potent H3 receptor ligand
6-(3-piperidin-1-ylpropoxy)pyridin-3-amine
-
50% inhibition at 0.053 mM, simultaneously a potent H3 receptor ligand
6-chloro-2-phenyl-4H-chromen-4-one
-
-
6-methyl-2-phenyl-4H-chromen-4-one
-
-
6-piperidin-1-yl-1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-hexan-1-one
-
50% inhibition at 0.0089 mM, simultaneously a highly potent H3 receptor ligand
7-chloro-4-(3-piperidin-1-ylpropoxy)quinoline
-
50% inhibition at 0.0026 mM, simultaneously a potent H3 receptor ligand
8-(3-(1H-imidazol-4-yl)propoxy)-5-nitroquinoline
-
50% inhibition at 0.0117 mM, simultaneously a highly potent H3 receptor ligand
8-bromo-6-chloro-2-phenyl-4H-chromen-4-one
-
-
8-bromo-6-methyl-2-phenyl-4H-chromen-4-one
-
-
amodiaquine
Biogenic amines
-
-
-
bromo-lysergic acid diethylamide
-
55% inhibition at 0.005 mM
Bufotenine
-
-
chlorpromazine
d-Chlorpheniramine
-
-
Dimaprit
-
-
diphenhydramine
potent HNMT inhibitor, occupies the histamine-binding site, thus blocks access to the enzyme’s active site
ethylamine
-
-
histamine
Impromidine
-
competitive, reversible
iodoacetamide
Methylhistamine
methylthioadenosine
-
-
Metoprine
N-(2-(1H-imidazol-4-yl)ethyl)-1,2,3,4-tetrahydroacridin-9-amine
-
50% inhibition at 0.000086 mM, simultaneously a highly potent H3 receptor ligand
N-(2-(1H-imidazol-4-yl)ethyl)-N-methylquinolin-4-amine
-
50% inhibition at 0.000079 mM, simultaneously a highly potent H3 receptor ligand
N-(2-(1H-imidazol-4-yl)ethyl)quinolin-4-amine
-
50% inhibition at 0.000055 mM, simultaneously a highly potent H3 receptor ligand
N-(3-(1H-imidazol-4-yl)propyl)-1,2,3,4-tetrahydroacridin-9-amine
-
50% inhibition at 0.000035 mM, simultaneously a highly potent H3 receptor ligand
N-(3-(1H-imidazol-4-yl)propyl)-2-methylquinolin-4-amine
-
50% inhibition at 0.000054 mM, simultaneously a highly potent H3 receptor ligand
N-(3-(1H-imidazol-4-yl)propyl)-N-methylquinolin-4-amine
-
50% inhibition at 0.000035 mM, simultaneously a highly potent H3 receptor ligand
N-(3-(1H-imidazol-4-yl)propyl)quinolin-4-amine
-
50% inhibition at 0.000024 mM, simultaneously a highly potent H3 receptor ligand
N-ethylmaleimide
-
-
N-[2(benzhydryloxy)ethyl] N N-dimethylamine
-
diphenhydramine, competitive inhibitor
N2-[2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-ethyl]-pyridine-2,5-diamine
-
50% inhibition at 0.00031 mM, simultaneously a highly potent H3 receptor ligand
N2-[3-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propyl]-pyridine-2,5-diamine
-
50% inhibition at 0.0013 mM, simultaneously a highly potent H3 receptor ligand
N2-[4-[4-(3-piperidin-1-yl-propoxy)-phenyl]-butyl]-pyridine-2,5-diamine
-
50% inhibition at 0.00034 mM, simultaneously a highly potent H3 receptor ligand
Nalpha-methylhistamine
-
weak
p-chloromercuribenzoate
p-hydroxymercuribenzoate
-
complete inhibition at 0.1 mM
S-adenosylhomocysteine
serotonin
SKF 91488
tacrine
tryptamine
-
and the hydroxyl derivative
Tubocurare
-
-
tyramine
-
and the hydroxyl derivative
[4-(3-piperidin-1-yl-propoxy)-phenyl]-(1-quinolin-4-yl-piperidin-4-yl)-methanone
-
50% inhibition at 0.00031 mM, simultaneously a highly potent H3 receptor ligand
additional information
-