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2.7.1.1: hexokinase

This is an abbreviated version!
For detailed information about hexokinase, go to the full flat file.

Word Map on EC 2.7.1.1

Reaction

ATP
+
D-glucose
=
ADP
 +
D-glucose 6-phosphate

Synonyms

6-phosphate glucose kinase, AtHXK1, ATP-D-hexose 6-phosphotransferase, ATP-D-hexose-6-phosphotransferase, ATP-dependent hexokinase, ATP: D-glucose 6-phosphotransferase, ATP: D-hexose 6-phosphotransferase, ATP:D-glucose 6-phosphotransferase, ATP:D-hexose 6-phosphotransferase, BmHk, brain form hexokinase, CzHXK1, FgHXK1, FgHXK2, GCK, GK, GKbeta, GlcK, glk, GlkB, glucokinase, glucokinase 1, glucokinase B, glucose ATP phosphotransferase, HaHXK1, hexokinase, hexokinase (phosphorylating), hexokinase 1, hexokinase 2, hexokinase 3, hexokinase 6, hexokinase A, hexokinase D, hexokinase Dor, hexokinase I, hexokinase II, hexokinase III, hexokinase IV, hexokinase PI, hexokinase PII, hexokinase type I, hexokinase type II, hexokinase type IV, hexokinase type IV glucokinase, hexokinase, tumor isozyme, hexokinase-1, hexokinase-10, hexokinase-2, hexokinase-4, hexokinase-5, hexokinase-6, hexokinase-7, hexokinase-8, hexokinase-9, hexokinase-II, hexokinase-like 1, hGK, hGK isoform 1, HK, HK II, HK-1, HK-I, HK-R, HK1, HK2, HK4, HKDC1, HKI, HKII, HKIII, HKL1, HPGLK1, HXK, HXK A, HXK II, Hxk1, HXK10, Hxk2, Hxk3, HXK4, HXK5, HXK6, HXK7, HXK8, HXK9, hxkC, hxkD, kinase, hexo- (phosphorylating), KlHxk1, LGK, LGK2, liver glucokinase, liver glucokinase isoform 2, MODY2 glucokinase, More, muscle form hexokinase, NfGlck, NtHXK1, OsHXK, OsHXK1, OsHXK10, OsHXK2, OsHXK3, OsHXK4, OsHXK5, OsHXK6, OsHXK7, OsHXK9, pHXK, plastid hexokinase, PpHXK1, PpHXK10, PpHXK11, PpHXK2, PpHXK3, PpHXK4, PpHXK5, PpHXK6, PpHXK7, PpHXK8, PpHXK9, Rag5p, ROK hexokinase, ScHK2, ScHXK2, SoHXK1, StHK, STK_23540, StoHK, TbHK1, TbHK2, TcHK, TthHK, type II hexokinase, VIT_18s0001g14230, xprF, Zm.5206, Zm.95484

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.1 hexokinase

Activating Compound

Activating Compound on EC 2.7.1.1 - hexokinase

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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2E)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)phenyl]-N-[4-(1,2-dihydroxyethyl)-1,3-thiazol-2-yl]prop-2-enamide
-
-
(2R)-2-[4-(cyclopropylsulfonyl)phenyl]-N-(5-fluorothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
96% maximum activation above control at 6.5 mM glucose
(2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide
-
activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator
(2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide}
-
RO0281675, 1.5fold change in Vmax or kcat at 0.003 mM
(6-ethoxyquinazolin-4-yl)(1-methyl-1H-pyrazol-3-yl)amine
-
increases glucokinase activity at glucose concentrations up to approximately 20 mM
(6-ethoxyquinazolin-4-yl)pyridin-2-ylamine
-
increases glucokinase activity at glucose concentrations below approximately 7 mM
(6-isopropoxyquinazolin-4-yl)(1-methyl-1H-pyrazol-3-yl)amine
-
increases glucokinase activity at glucose concentrations up to approximately 20 mM
(R)-2-(4-(methylsulfonyl)phenyl)-3-((R)-3-oxocyclopentyl)-N-(pyrazin-2-yl)propanamide
-
piragliatin
(S)-2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-fluorothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
PSN-GK1, 1.1fold change in Vmax or kcat at 0.0001 mM
(S)-2-[3-chloro-4-(ethylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
26% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-(4,4-difluorocyclohexyl)-N-(5-methylpyridin-2-yl)propanamide
-
15% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclobutyl-N-(5-methylpyridin-2-yl)propanamide
-
72% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclohexyl-N-(5-methylpyridin-2-yl)propanamide
-
46% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide
-
57% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-4-methyl-N-(5-methylpyridin-2-yl)pentanamide
-
37% maximum activation above control at 6.5 mM glucose
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)-3-phenylpropanamide
-
30% maximum activation above control at 6.5 mM glucose
(S)-2-[4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide
-
67% maximum activation above control at 6.5 mM glucose
(S)-2-[4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-pyrazin-2-ylpropanamide
-
66% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide
-
67% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide
-
84% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide
-
122% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-chloropyridin-2-yl)-3-cyclopentylpropanamide
-
82% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide
-
57% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyrazin-2-yl)propanamide
-
104% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide
-
69% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-1,3-thiazol-2-ylpropanamide
-
42% maximum activation above control at 6.5 mM glucose
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-1H-pyrazol-3-ylpropanamide
-
50% maximum activation above control at 6.5 mM glucose
(S)-3-(4-((3-fluoropyrrolidin-1-yl)sulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(thiazol-2-yl)benzamide
-
activation: 1.9fold
(S)-3-(4-((3-fluoropyrrolidin-1-yl)sulfonyl)phenoxy)-N-(5-fluorothiazol-2-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 2.2fold
(S)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide
-
76% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-pyrazin-2-ylpropanamide
-
94% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[4-(ethylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide
-
73% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide
-
65% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-pyridin-2-ylpropanamide
-
43% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-[5-(trifluoromethyl)pyridin-2-yl]propanamide
-
35% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[5-methyl-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide
-
103% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-2-[5-methyl-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide
-
48% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-N-(5-methylpyrazin-2-yl)-2-[4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]propanamide
-
101% maximum activation above control at 6.5 mM glucose
(S)-3-cyclopentyl-N-(5-methylpyridin-2-yl)-2-[4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]propanamide
-
58% maximum activation above control at 6.5 mM glucose
(S)-6-(3-cyclopentyl-2-[4-(trifluoromethyl)-1H-imidazol-1-yl]propanamido)nicotinic acid
-
in the presence of liver-specific GKA, progress curves at 1 mM glucose are similar to those at 5 mM, reflecting activation of GK. With steady-state kinetic methods it is shown that there are at least two kinetically distinct forms of glucokinase that interconvert through a slow conformational change and that this interconversion is affected by glucose concentration and a liver-specific GKA
(Z)-2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-(2-methylpropylidene)-4-oxo-4,5-dihydro thiazol-2-yl)-3-(tetrahydro-2Hpyran-4-yl)propanamide
-
activation: 1.17fold
(Z)-N-(5-benzylidene-4-oxo-4,5-dihydrothiazol-2-yl)-2-(4-(cyclopropylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.24fold
1-(1-(4-chlorophenyl)cyclohexyl)-3-(thiazol-2-yl)urea
-
-
1-[6'-(2-hydroxy-2-methylpropoxy)-4-[(5-methylpyridin-3-yl)oxy]-3,3'-bipyridin-6-yl]-3-methylurea
i.e. AM-2394. Compound activates glucokinase with an EC50 of 60 nM, increases the affinity of glucokinase for glucose by approximately 10fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes
2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-N,N-dimethyl-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxamide
-
maximal activation: 2.35fold
2-(4-(cyclopropylsulfonyl)phenyl)-3-(tetrahydro-2Hpyran-4-yl)-N-(4,5,6,7-tetrahydrobenzo[d]thiazol-2-yl)propanamide
-
activation: 2.27fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(4-(prop-1-en-2-yl)thiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 2.4fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(4-isopropylthiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 2.97fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(4-oxo-4,5-dihydrothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.65fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(5,6-dihydro-4Hcyclopenta[d]thiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 3.4fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-iodo-4-isopropylthiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.34fold
2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c] pyridin-2-yl)-3-(tetrahydro-2Hpyran-4-yl)propanamide
-
activation: 2.26fold
2-(4-(methylsulfonyl)phenyl)-N-(4-phenylthiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)-propanamide
-
activation: 1.3fold
2-(methylamino)-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
-
2-amino-4-chloro-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-4-fluoro-5-((1-methyl-1H-imidazol-2-yl)thio)-N-(thiazol-2-yl)benzamide
2-amino-4-fluoro-5-(1,3,4-thiadiazol-2-ylsulfanyl)-N-(3-trifluoromethyl-phenyl)-benzamide
-
1.14fold activation at 0.01 mM
2-amino-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-N-(3-trifluoromethyl-phenyl)-benzamide
-
1.47fold activation at 0.01 mM
2-amino-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-N-thiazol-2-yl-benzamide
2-amino-4-fluoro-5-(4-methyl-thiazol-2-ylsulfanyl)-N-(3-trifluoromethyl-phenyl)-benzamide
-
0.89fold activation at 0.01 mM
2-amino-4-fluoro-5-(thiazol-2-ylsulfanyl)-N-(3-trifluoromethyl-phenyl)-benzamide
-
1.15fold activation at 0.01 mM
2-amino-4-fluoro-5-[(1-methyl-1H-imidazol-2-yl)sulfanyl]-N-(4-methylthiazol-2-yl)benzamide
-
108% maximum activation above control at 6.5 mM glucose
2-amino-4-fluoro-N-(3-fluoro-phenyl)-5-(1,3,4-thiadiazol-2-ylsulfanyl)-benzamide
-
1.36fold activation at 0.01 mM
2-amino-4-fluoro-N-(3-fluoro-phenyl)-5-(1-methyl-1Himidazol-2-ylsulfanyl)-benzamide
-
2.04fold activation at 0.01 mM
2-amino-4-fluoro-N-(3-fluoro-phenyl)-5-(pyridin-2-ylsulfanyl)-benzamide
-
1.1fold activation at 0.01 mM
2-amino-4-fluoro-N-(3-fluoro-phenyl)-5-(thiazol-2-ylsulfanyl)-benzamide
-
1.25fold activation at 0.01 mM
2-amino-4-fluoro-N-(3-methoxy-phenyl)-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-benzamide
-
1.15fold activation at 0.01 mM
2-amino-4-fluoro-N-(4-methoxy-phenyl)-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-benzamide
-
2.01fold activation at 0.01 mM
2-amino-5-((4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-(5-methylthiazol-2-yl)benzamide
-
1.3fold change in Vmax or kcat at 0.01 mM
2-amino-5-(1H-imidazol-2-ylsulfanyl)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-(2-fluorophenoxy)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-(2-methoxyphenoxy)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-(3-fluorophenoxy)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-(4-fluorophenoxy)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-(benzoxazol-2-ylsulfanyl)-4-fluoro-N-(3-fluoro-phenyl)-benzamide
-
0.83fold activation at 0.01 mM
2-amino-5-(ethylsulfanyl)-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-chloro-N-(1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-chloro-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-ethoxy-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-[(1-methyl-1H-imidazol-2-yl)sulfanyl]-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(1,2,4-thiadiazol-5-yl)benzamide
-
-
2-amino-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(1,3-thiazol-2-yl)benzamide
-
-
2-amino-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-N-[4-(trifluoromethyl)-1,3-thiazol-2-yl]benzamide
-
-
2-amino-5-[2-[methyl(methylidene)oxido-l6-sulfanyl]phenoxy]-N-(4-methyl-1,3-thiazol-2-yl)benzamide
-
-
2-amino-N-(1,3-thiazol-2-yl)benzamide
-
-
2-amino-N-(3,4-dimethoxy-phenyl)-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-benzamide
-
1.32fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-4-fluoro-5-(1,3,4-thiadiazol-2-ylsulfanyl)-benzamide
-
1.22fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-benzamide
-
2.09fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-4-fluoro-5-(4-methylthiazol-2-ylsulfanyl)-benzamide
-
1.1fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-4-fluoro-5-(pyridin-2-ylsulfanyl)-benzamide
-
1.12fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-4-fluoro-5-(thiazol-2-ylsulfanyl)-benzamide
-
1.21fold activation at 0.01 mM
2-amino-N-(3-amino-phenyl)-5-(4,6-dimethyl-pyrimidin-2-ylsulfanyl)-4-fluoro-benzamide
-
1.09fold activation at 0.01 mM
2-amino-N-(3-aminomethyl-phenyl)-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-benzamide
-
1.01fold activation at 0.01 mM
2-amino-N-(3-cyano-phenyl)-4-fluoro-5-(1,3,4-thiadiazol-2-ylsulfanyl)-benzamide
-
1.2fold activation at 0.01 mM
2-amino-N-(3-cyano-phenyl)-4-fluoro-5-(1-methyl-1Himidazol-2-ylsulfanyl)-benzamide
-
1.95fold activation at 0.01 mM
2-amino-N-(3-cyano-phenyl)-4-fluoro-5-(4-methylthiazol-2-ylsulfanyl)-benzamide
-
0.99fold activation at 0.01 mM
2-amino-N-(3-cyano-phenyl)-4-fluoro-5-(thiazol-2-ylsulfanyl)-benzamide
-
1.2fold activation at 0.01 mM
2-amino-N-(3-cyano-phenyl)-5-(4,6-dimethyl-pyrimidin-2-ylsulfanyl)-4-fluoro-benzamide
-
1.01fold activation at 0.01 mM
2-amino-N-(3-methyl-1,2,4-thiadiazol-5-yl)-5-(phenylsulfanyl)benzamide
-
-
2-amino-N-(3-methyl-1,2,4-thiadiazol-5-yl)-5-(pyridin-2-ylsulfanyl)benzamide
-
-
2-amino-N-(3-methyl-1,2,4-thiadiazol-5-yl)-5-(pyridin-3-ylsulfanyl)benzamide
-
-
2-amino-N-(3-methyl-1,2,4-thiadiazol-5-yl)-5-(pyridin-4-ylsulfanyl)benzamide
-
-
2-amino-N-(3-methyl-1,2,4-thiadiazol-5-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
-
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-(4H-1,2,4-triazol-3-ylsulfanyl)benzamide
-
-
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-(phenylsulfanyl)benzamide
-
-
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-(pyridin-2-ylsulfanyl)benzamide
-
-
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
2-amino-N-(4-methylthiazol-2-yl)-5-phenoxybenzamide
-
-
2-amino-N-(5-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
-
2-amino-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
-
2-cyclopentyl-1-(4-(methylsulfonyl)phenyl)-N-(thiazol-2-yl)ethanesulfonamide
-
-
2-[(3-cyclopentyl-2-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]propanoyl)amino]-5-methoxy-1H-[1,3]thiazolo[5,4-b]pyridin-3-ium
-
-
2-[4-(2,4-difluoro-phenyl)-piperazin-1-yl]-N-(3,4-dimethoxy-phenyl)-acetamide
-
1.01fold activation at 0.01 mM
2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-N-(3-trifluoromethyl-phenyl)-acetamide
-
1.06fold activation at 0.01 mM
2-[4-(methylsulfonyl)phenyl]-3-(tetrahydro-2H-pyran-4-yl)-N-(1,3-thiazol-2-yl)propanamide
-
activation: 2.45fold
28-homobrassinolide
28-homobrassinolide is able to protect or restore the native structure of hexokinase when exposed to diabetic levels of glucose. The denatured hexokinase is renatured upon binding with homobrassinolide. Homobrassinolide is able to bind to the drug-binding pocket of glucokinase. The glide energy is -7.1 kcal/mol
3-((3-methylbut-2-en-1-yl)oxy)-5-(4-(morpholinosulfonyl)phenoxy)-N-(thiazol-2-yl)benzamide
-
activation: 2.1fold
3-(4-(((2S,6R)-2,6-dimethylmorpholino)sulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(thiazol-2-yl)benzamide
-
activation: 1.5fold
3-(4-(((2S,6R)-2,6-dimethylmorpholino)sulfonyl)phenoxy)-N-(5-fluorothiazol-2-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 1.7fold
3-(4-((4-methoxypiperidin-1-yl)sulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(thiazol-2-yl)benzamide
-
activation: 1.7fold
3-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(thiazol-2-yl)benzamide
-
activation: 1.7fold
3-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)phenoxy)-N-(5-fluorothiazol-2-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 1.9fold
3-(4-(cyclopropylsulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(4-oxo-4,5-dihydrothiazol-2-yl)benzamide
-
activation: 1.5fold
3-(4-(cyclopropylsulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(5-methylpyrazin-2-yl)benzamide
-
activation: 1.6fold
3-(4-(cyclopropylsulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)-N-(thiazol-2-yl)benzamide
-
activation: 2.4fold
3-(4-(cyclopropylsulfonyl)phenoxy)-N-(1,5-dimethyl-1H-pyr-azol-3-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 1.5fold
3-(4-(cyclopropylsulfonyl)phenoxy)-N-(4-(4-fluorophenyl)thiazol-2-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 0.9fold
3-(4-(cyclopropylsulfonyl)phenoxy)-N-(5-fluorothiazol-2-yl)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 1.8fold
3-(5-chloro-1,3-thiazol-2-yl)-1-[4-(methylsulfonyl)phenyl]-1-(thiophen-2-ylmethyl)urea
-
-
3-(5-chlorothiazol-2-yl)-1-(4-(methylsulfonyl)phenyl)-1-(thiophen-3-ylmethyl)urea
-
-
3-amino-N-[2-amino-4-fluoro-5-(1-methyl-1H-imidazol-2-ylsulfanyl)-phenyl]-benzamide
-
1.16fold activation at 0.01 mM
3-phosphoglycerate
-
activates
3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)benzamide
-
maximal activation: 2.2fold
3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]-N-[5-(2-oxo-1,2-dihydropyridin-4-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.13fold
3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]-N-[5-(pyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 1.92fold
3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]-N-[5-(pyrimidin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.35fold
3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]-N-[5-(pyrimidin-4-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.53fold
3-[4-(azetidine-1-carbonyl)phenoxy]-N-[5-(2-hydroxyethyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamide
-
maximal activation: 1.97fold
3-[4-(azetidine-1-carbonyl)phenoxy]-N-[5-(2-methoxyethyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamide
-
maximal activation: 1.76fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)benzamide
-
maximal activation: 3.42fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)benzamide
-
maximal activation: 3.41fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-(5-phenyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)benzamide
-
maximal activation: 2.05fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-(7-oxo-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)benzamide
-
maximal activation: 2.61fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-[5-(propan-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-[5-(pyridin-2-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.39fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-[5-(pyridin-3-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.7fold
3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]-N-[5-(pyridin-4-yl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]benzamide
-
maximal activation: 2.97fold
4-[4-(dimethylcarbamoyl)-3-fluorophenoxy]-2-ethyl-2-methyl-N-(5-methylpyridin-2-yl)-2,3-dihydro-1-benzofuran-6-carboxamide
-
-
5-(2-methylpropyl)-N-(1,3-thiazol-2-yl)-1H-indazol-3-amine
-
-
5-({3-(propan-2-yloxy)-5-[2-(thiophen-3-yl)ethoxy]benzoyl}amino)-1,3,4-thiadiazole-2-carboxylic acid
-
-
6-(3-(((S)-1-methoxypropan-2-yl)oxy)-5-(((S)-1-phenylpropan-2-yl)oxy)benzamido)nicotinic acid
6-({3-(propan-2-yloxy)-5-[2-(thiophen-3-yl)ethoxy]benzoyl}amino)pyridine-3-carboxylic acid
-
GKA22
6-ethoxy-N-(1-methyl-1H-pyrrol-3-yl)-quinazolin-4-amine
-
0.95fold change in Vmax or kcat at 0.05 mM
6-ethoxy-N-(pyridin-2-yl)-quinazolin-4-amine
-
0.62fold change in Vmax or kcat at 0.05 mM
6-isopropoxy-N-(1-methyl-1H-pyrrol-3-yl)quinazolin-4-amine
-
0.8fold change in Vmax or kcat at 0.05 mM
6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase
-
6-[[3-hydroxy-5-(propan-2-yloxy)benzoyl]amino]pyridine-3-carboxylic acid
-
activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator
6-{[3-(2-methylpropoxy)-5-(propan-2-yloxy)benzoyl]amino}pyridine-3-carboxylic acid
-
-
alpha-D-glucose
-
bad peptide
-
-
-
citrate
-
allosteric activator
ethyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.22fold
ethyl 2-[([2-amino-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]phenyl]carbonyl)amino]-1,3-thiazole-4-carboxylate
-
-
fructose
-
-
galactose
-
activates isoenzyme Hex II
GKA50
glucokinase-associated phosphatase
-
-
-
glucokinase-associated protein
-
glucose 6-phosphate
-
recombinant HXK1: at 10 mM 13% activation, at 20 mM 31% activation, recombinant HXK2: at 10 mM 23% activation, at 20 mM 48% activation
glucose-6-phosphate
Q56VN6
10 mM, recombinant enzyme is 3fold activated
glycerol 3-phosphate
-
influences enzyme activity at pH 6.5 by preventing substrate and product inhibition by ATP and ADP, respectively
Insulin
-
stimulating effect is abolished when lactate is added
-
isocitrate
-
activates isoenzyme Hex II
LY-2121260
lyxose
-
activates isoenzyme Hex II
mannose 6-phosphate
-
activates isoenzyme Hex II
methyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.38fold
N,N'-bis-(2-methoxy-phenyl)-isophthalamide
-
1.02fold activation at 0.01 mM
N,N'-bis-(3-methoxy-phenyl)-isophthalamide
-
0.81fold activation at 0.01 mM
N,N'-bis-(4-methoxy-phenyl)-isophthalamide
-
0.89fold activation at 0.01 mM
N,N-dicyclohexyl-N'-methyldicarbonimidic diamide
-
-
N-(3-amino-phenyl)-2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-acetamide
-
1.08fold activation at 0.01 mM
N-(3-cyano-phenyl)-2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-acetamide
-
0.96fold activation at 0.01 mM
N-(3-fluoro-phenyl)-2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-acetamide
-
1.01fold activation at 0.01 mM
N-(4,5-dimethylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.72fold
N-(4-(4-fluorophenyl)thiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.25fold
N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.22fold
N-(4-(tert-butyl)thiazol-2-yl)-3-(4-(cyclopropylsulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 0.7fold
N-(4-cyclopropylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.87fold
N-(4-ethylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)-propanamide
-
activation: 2.17fold
N-(4-isobutylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)-propanamide
-
activation: 2.05fold
N-(4-isopropylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)-propanamide
-
activation: 2.49fold
N-(4-methyl-1,3-thiazol-2-yl)-3-(pyridin-3-ylmethoxy)pyridin-2-amine
-
-
N-(4-methyl-1,3-thiazol-2-yl)-3-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
-
N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-2-nitrobenzamide
-
-
N-(4-tert-butylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)-propanamide
-
activation: 1.29fold
N-(5,6-dihydro-4H-cyclopenta[d][1,3]thiazol-2-yl)-3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamide
-
maximal activation: 4.8fold
N-(5-acetyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamide
-
maximal activation: 2.5fold
N-(5-benzyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamide
-
maximal activation: 2.1fold
N-(5-bromo-4-isopropylthiazol-2-yl)-2-(4-(cyclopropylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.67fold
N-(5-ethyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamide
-
maximal activation: 2.08fold
N-(5-fluorothiazol-2-yl)-3-((3-methylbut-2-en-1-yl)oxy)-5-(4-(morpholinosulfonyl)phenoxy)benzamide
-
activation: 1.8fold
N-(5-fluorothiazol-2-yl)-3-(4-((4-methoxypiperidin-1-yl)sulfonyl)phenoxy)-5-((3-methylbut-2-en-1-yl)oxy)benzamide
-
activation: 1.7fold
N-(5-isopropyl-4-methylthiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.13fold
N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamide
-
maximal activation: 2.17fold
N-(6-fluorobenzo[d]thiazol-2-yl)-2-(4-(methylsulfonyl)phenyl)-3-(tetrahydro-2H-pyran-4-yl)propanamide
-
activation: 1.3fold
N-[2-amino-4-fluoro-5-[(1-methyl-1H-imidazol-2-yl)sulfanyl]benzyl]-1,3-thiazol-2-amine
-
addition of 0.02 mM N-[2-amino-4-fluoro-5-[(1-methyl-1H-imidazol-2-yl)sulfanyl]benzyl]-1,3-thiazol-2-amine results in the loss of positive cooperativity with glucose and in activation of glucokinase catalysis increasing both kcat and the apparent glucose affinity
pentaubiquitin
-
PF-04937319
-
maximal activation: 2.11fold
phosphate
-
activates
phosphoenolpyruvate
-
activates isoenzyme Hex I
polyubiquitin
-
propionyl-CoA carboxylase beta-subunit
-
-
-
ribose
-
activates isoenzyme Hex II
RO-0275145
-
-
RO-0281675
RO-1440
-
148% maximum activation above control at 6.5 mM glucose
RO-28-0450
-
racemic, activates the enzyme
RO-28-1675
RO-281675
-
-
RO-4389620
-
also known as R1440, GK2, or piragliatin
RO0274375
-
wild-type enzyme V62A, V62T, and V62L respond to the activator. V62Q, V62E, V62F, and V62K are resistant to the activators
RO0281675
-
wild-type enzyme V62A, V62T, and V62L respond to the activator. V62Q, V62E, V62F, and V62K are resistant to the activators
RO0283946
-
wild-type enzyme V62A, V62T, and V62L respond to the activator. V62Q, V62E, V62F, and V62K are resistant to the activators
-
tert-butyl (S)-2-(3-(4-(azetidine-1-carbonyl)phenoxy)-5-((1-methoxypropan-2-yl)oxy)benzamido)-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate
-
glucokinase activators are being developed for the treatment of type 2 diabetes mellitus. Glucokinase activators have risks of hypoglycemia caused by over-activation of glucokinase in islet cells and dyslipidemia caused by over-activation of intrahepatic glucokinase. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of glucokinase activator. tert-Butyl (S)-2-(3-(4-(azetidine-1-carbonyl)phenoxy)-5-((1-methoxypropan-2-yl)oxy)benzamido)-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate shows a good balance between in vitro potency and enzyme kinetic parameters, and protects beta-cells from streptozotocin-induced apoptosis. Chronic treatment of this compound demonstrates its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test. Acute treatment of this compound does not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)-3-fluorophenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.83 fold
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2R)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.96fold
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-hydroxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.62fold
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.65fold
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[5,4-b]pyridine-4(5H)-carboxylate
-
maximal activation: 1.8fold
tert-butyl 2-(3-[4-(azetidine-1-carbonyl)phenoxy]-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido)-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.84fold
tert-butyl 2-(3-[[6-(azetidine-1-carbonyl)pyridin-3-yl]oxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.1fold
tert-butyl 2-(3-[[6-(methanesulfonyl)pyridin-3-yl]oxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 4.07fold
tert-butyl 2-[3-(3,5-difluorophenoxy)-5-[[(2S)-1-methoxypropan-2-yl]oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.72fold
tert-butyl 2-[3-(benzyloxy)-5-[4-(methanesulfonyl)phenoxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.3fold
tert-butyl 2-[3-(cyclohexyloxy)-5-[4-(methanesulfonyl)phenoxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 1.71fold
tert-butyl 2-[3-(cyclopentylmethoxy)-5-[4-(methanesulfonyl)phenoxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.11fold
tert-butyl 2-[3-(cyclopentyloxy)-5-[4-(methanesulfonyl)phenoxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 3.17fold
tert-butyl 2-[3-[2-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 1.89fold
tert-butyl 2-[3-[3-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.74fold
tert-butyl 2-[3-[4-(azetidine-1-carbonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.89fold
tert-butyl 2-[3-[4-(azetidine-1-sulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 3.26fold
tert-butyl 2-[3-[4-(cyclopropanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 3.12fold
tert-butyl 2-[3-[4-(dimethylcarbamoyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 1.91fold
tert-butyl 2-[3-[4-(ethanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.37fold
tert-butyl 2-[3-[4-(methanesulfonyl)phenoxy]-5-(2-methoxyethoxy)benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.3fold
tert-butyl 2-[3-[4-(methanesulfonyl)phenoxy]-5-[(1-methoxypropan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[5,4-c]pyridine-5(4H)-carboxylate
-
maximal activation: 2.94fold
tert-butyl 2-[3-[4-(methanesulfonyl)phenoxy]-5-[(propan-2-yl)oxy]benzamido]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridine-5(4H)-carboxylate
-
maximal activation: 3.55fold
xylose
-
activates isoenzyme Hex II
additional information
-