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Literature summary extracted from

  • Zheng, W.; Padia, J.; Urban, D.J.; Jadhav, A.; Goker-Alpan, O.; Simeonov, A.; Goldin, E.; Auld, D.; LaMarca, M.E.; Inglese, J.; Austin, C.P.; Sidransky, E.
    Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease (2007), Proc. Natl. Acad. Sci. USA, 104, 13192-13197.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.45 (1R,2R,3S,4S,5R,6S)-7-oxabicyclo[4.1.0]heptane-2,3,4,5-tetrol
-
 Homo sapiens
3.2.1.45 2-(4-(5-chloro-2-methoxyphenylamino)-6-(pyrrolidin-1-yl)-1,3,5-triazin-2-ylamino)ethanol
-
 Homo sapiens
3.2.1.45 2-([4-[(3-methylphenyl)amino]-6-morpholin-4-yl-1,3,5-triazin-2-yl]amino)ethanol
-
 Homo sapiens
3.2.1.45 2-([4-[(3-methylphenyl)amino]-6-pyrrolidin-1-yl-1,3,5-triazin-2-yl]amino)ethanol
-
 Homo sapiens
3.2.1.45 2-([4-[(4-chlorophenyl)amino]-6-morpholin-4-yl-1,3,5-triazin-2-yl]amino)ethanol
-
 Homo sapiens
3.2.1.45 2-([4-[(4-chlorophenyl)amino]-6-pyrrolidin-1-yl-1,3,5-triazin-2-yl]amino)ethanol
-
 Homo sapiens
3.2.1.45 2-[[4-(prop-2-en-1-ylamino)-6-pyrrolidin-1-yl-1,3,5-triazin-2-yl]amino]ethanol
-
 Homo sapiens
3.2.1.45 4-methyl-N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)cyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 4-methyl-N-(4-methyl-2-piperidin-1-ylquinolin-6-yl)cyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 4-methyl-N-[4-methyl-2-(4-methylpiperidin-1-yl)quinolin-6-yl]cyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 4-methyl-N-[4-methyl-2-(4-pyrimidin-4-ylpiperazin-1-yl)-1,2-dihydroquinolin-6-yl]cyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 4-[[(4-chlorophenyl)sulfonyl]amino]-N-(2,5-dihydro-1,3-thiazol-2-yl)benzamide
-
 Homo sapiens
3.2.1.45 isofagomine
-
 Homo sapiens
3.2.1.45 N-(2,5-dihydro-1,3-thiazol-2-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)-4-propylcyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)cyclopropanecarboxamide
-
 Homo sapiens
3.2.1.45 N-(4-methyl-2-morpholinoquinolin-6-yl)cyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 N-(5-ethyl-1,3,4-thiadiazol-2-yl)-4-(phenylsulfonamido)benzamide
-
 Homo sapiens
3.2.1.45 N-(5-ethyl-1,3,4-thiadiazolidin-2-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-(5-methylisoxazol-3-yl)-4-(phenylsulfonamido)benzamide
-
 Homo sapiens
3.2.1.45 N-(5-methylisoxazol-3-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-benzyl-4-[(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-butyl-4-[(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-butyldeoxynojirimycin
-
 Homo sapiens
3.2.1.45 N-hydroxy-6-pyrrolidin-1-yl-1,3,5-triazine-2,4-diamine
-
 Homo sapiens
3.2.1.45 N-nonyldeoxynojirimycin
-
 Homo sapiens
3.2.1.45 N-phenyl-4-[(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
3.2.1.45 N-[2-(diethylamino)-4-methyl-1,2-dihydroquinolin-6-yl]-4-methylcyclohexanecarboxamide
-
 Homo sapiens
3.2.1.45 N-[2-[(3-chlorophenyl)amino]-4-methyl-1,2-dihydroquinolin-6-yl]-4-methylcyclohexanecarboxamide
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.2.1.45 0.862
-
 4-methylumbelliferyl-beta-D-glucopyranoside in 50 mM citric acid, KH2PO4 (pH 5.9), 10 mM sodium taurocholate, and 0.01% Tween 20, at 21°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.2.1.45 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.2.1.45 fibroblast
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.45 4-methylumbelliferyl-beta-D-glucopyranoside + H2O
-
 Homo sapiens methylumbelliferone + glucose
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.1.45 acid beta-glucosidase
-
 Homo sapiens
3.2.1.45 Cerezyme commercial preparation Homo sapiens
3.2.1.45 glucocerebrosidase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.2.1.45 0.000031
-
-
 Homo sapiens N-(4-methyl-2-morpholinoquinolin-6-yl)cyclohexanecarboxamide
3.2.1.45 0.000063
-
-
 Homo sapiens 4-methyl-N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)cyclohexanecarboxamide
3.2.1.45 0.000103
-
-
 Homo sapiens N-(5-ethyl-1,3,4-thiadiazol-2-yl)-4-(phenylsulfonamido)benzamide
3.2.1.45 0.000133
-
-
 Homo sapiens N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)-4-propylcyclohexanecarboxamide
3.2.1.45 0.000168
-
-
 Homo sapiens N-(5-methylisoxazol-3-yl)-4-(phenylsulfonamido)benzamide
3.2.1.45 0.000183
-
-
 Homo sapiens N-(4-methyl-2-morpholin-4-ylquinolin-6-yl)cyclopropanecarboxamide
3.2.1.45 0.000268
-
-
 Homo sapiens 4-methyl-N-[4-methyl-2-(4-methylpiperidin-1-yl)quinolin-6-yl]cyclohexanecarboxamide
3.2.1.45 0.00043
-
-
 Homo sapiens 2-(4-(5-chloro-2-methoxyphenylamino)-6-(pyrrolidin-1-yl)-1,3,5-triazin-2-ylamino)ethanol
3.2.1.45 0.000452
-
-
 Homo sapiens 4-methyl-N-(4-methyl-2-piperidin-1-ylquinolin-6-yl)cyclohexanecarboxamide
3.2.1.45 0.00106
-
-
 Homo sapiens N-[2-(diethylamino)-4-methyl-1,2-dihydroquinolin-6-yl]-4-methylcyclohexanecarboxamide
3.2.1.45 0.00129
-
-
 Homo sapiens 4-[[(4-chlorophenyl)sulfonyl]amino]-N-(2,5-dihydro-1,3-thiazol-2-yl)benzamide
3.2.1.45 0.00245
-
-
 Homo sapiens 4-methyl-N-[4-methyl-2-(4-pyrimidin-4-ylpiperazin-1-yl)-1,2-dihydroquinolin-6-yl]cyclohexanecarboxamide
3.2.1.45 0.00296
-
-
 Homo sapiens N-(5-ethyl-1,3,4-thiadiazolidin-2-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
3.2.1.45 0.00431
-
-
 Homo sapiens 2-([4-[(3-methylphenyl)amino]-6-pyrrolidin-1-yl-1,3,5-triazin-2-yl]amino)ethanol
3.2.1.45 0.00646
-
-
 Homo sapiens N-phenyl-4-[(phenylsulfonyl)amino]benzamide
3.2.1.45 0.00773
-
-
 Homo sapiens 2-([4-[(4-chlorophenyl)amino]-6-pyrrolidin-1-yl-1,3,5-triazin-2-yl]amino)ethanol
3.2.1.45 0.0167
-
-
 Homo sapiens (1R,2R,3S,4S,5R,6S)-7-oxabicyclo[4.1.0]heptane-2,3,4,5-tetrol
3.2.1.45 0.0246
-
-
 Homo sapiens N-butyl-4-[(phenylsulfonyl)amino]benzamide
3.2.1.45 0.0252
-
-
 Homo sapiens N-(5-methylisoxazol-3-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
3.2.1.45 0.0344
-
-
 Homo sapiens N-(2,5-dihydro-1,3-thiazol-2-yl)-4-[methyl(phenylsulfonyl)amino]benzamide
3.2.1.45 0.0465
-
-
 Homo sapiens 2-([4-[(4-chlorophenyl)amino]-6-morpholin-4-yl-1,3,5-triazin-2-yl]amino)ethanol
3.2.1.45 0.0477
-
-
 Homo sapiens 2-([4-[(3-methylphenyl)amino]-6-morpholin-4-yl-1,3,5-triazin-2-yl]amino)ethanol
3.2.1.45 0.1
-
 IC50 above 0.1 mM Homo sapiens N-benzyl-4-[(phenylsulfonyl)amino]benzamide