General Information of the Protein
Protein ID
PT02611
Protein Name
Ceramide glucosyltransferase
Secondarily
Protein Name
GLCT-1
Glucosylceramide synthase
Glycosylceramide synthase
UDP-glucose ceramide glucosyltransferase
UDP-glucose:N-acylsphingosine D-glucosyltransferase
Gene Name
UGCG
Sequence
MALLDLALEGMAVFGFVLFLVLWLMHFMAIIYTRLHLNKKATDKQPYSKLPGVSLLKPLKGVDPNLINNLETFFELDYPKYEVLLCVQDHDDPAIDVCKKLLGKYPNVDARLFIGGKKVGINPKINNLMPGYEVAKYDLIWICDSGIRVIPDTLTDMVNQMTEKVGLVHGLPYVADRQGFAATLEQVYFGTSHPRYYISANVTGFKCVTGMSCLMRKDVLDQAGGLIAFAQYIAEDYFMAKAIADRGWRFAMSTQVAMQNSGSYSISQFQSRMIRWTKLRINMLPATIICEPISECFVASLIIGWAAHHVFRWDIMVFFMCHCLAWFIFDYIQLRGVQGGTLCFSKLDYAVAWFIRESMTIYIFLSALWDPTISWRTGRYRLRCGGTAEEILDV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Participates in the initial step of the glucosylceramide-based glycosphingolipid/GSL synthetic pathway at the cytosolic surface of the Golgi (PubMed:8643456, PubMed:1532799). Catalyzes the transfer of glucose from UDP-glucose to ceramide to produce glucosylceramide/GlcCer (such as beta-D-glucosyl-(1<->1')-N-acylsphing-4-enine) (PubMed:1532799, PubMed:8643456). GlcCer is the core component of glycosphingolipids/GSLs, amphipathic molecules consisting of a ceramide lipid moiety embedded in the outer leaflet of the membrane, linked to one of hundreds of different externally oriented oligosaccharide structures (PubMed:8643456). Glycosphingolipids are essential components of membrane microdomains that mediate membrane trafficking and signal transduction, implicated in many fundamental cellular processes, including growth, differentiation, migration, morphogenesis, cell-to-cell and cell-to-matrix interactions (By similarity). They are required for instance in the proper development and functioning of the nervous system (By similarity). As an example of their role in signal transduction, they regulate the leptin receptor/LEPR in the leptin-mediated signaling pathway (By similarity). They also play an important role in the establishment of the skin barrier regulating keratinocyte differentiation and the proper assembly of the cornified envelope (By similarity). The biosynthesis of GSLs is also required for the proper intestinal endocytic uptake of nutritional lipids (By similarity). Catalyzes the synthesis of xylosylceramide/XylCer (such as beta-D-xylosyl-(1<->1')-N-acylsphing-4-enine) using UDP-Xyl as xylose donor (PubMed:33361282).
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Uniprot ID
Primary ID:
Q16739

Secondarily ID:
Q5T258
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Ensembl ID
ENSG00000148154
HGNC ID
HGNC:12524
Subcellular Location
Golgi apparatus membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0236110
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-(2,3-dihydro-1,4-benzodioxin-6-ylmethoxy)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
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C30H30ClF3N4O6
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0075555
N-[(1R,2S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]nonanamide
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C24H38N2O4
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0091328
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-1-(4-methylpiperazin-1-yl)-1-oxo-3-phenylmethoxypropan-2-yl]pyridine-3-carboxamide
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C28H28ClF3N4O4
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0191300
N-[(1R,2S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]octanamide
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C23H36N2O4
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0368789
N-[(2S)-1-[(1R,5S)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C26H27Cl4N3O2
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0443642
N-[(2S)-3-(4-chlorophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H26Cl3N3O2
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0075556
N-[(2R)-1-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-1-oxo-3-phenylmethoxypropan-2-yl]-2-[2-chloro-4-(trifluoromethyl)phenoxy]pyridine-3-carboxamide
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C30H30ClF3N4O4
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0443643
1-(2,4-dichlorophenyl)-N-[(2S)-3-(2,4-dichlorophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C24H25Cl4N3O2
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0070455
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-1-[(3R)-3-(methylamino)pyrrolidin-1-yl]-1-oxo-3-phenylmethoxypropan-2-yl]pyridine-3-carboxamide
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C28H28ClF3N4O4
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0057863
1-(2,4-dichlorophenyl)-N-[(2S)-3-(1H-indol-3-yl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C26H28Cl2N4O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0057860
N-[(2S)-1-[(1S,5R)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]-1-[4-(trifluoromethoxy)phenyl]cyclopropane-1-carboxamide
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C27H28Cl2F3N3O3
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0413929
N-[(2S)-3-(4-bromophenyl)-1-[2-(dimethylamino)ethyl-methylamino]-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H28BrCl2N3O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0264143
N-[(2R)-1-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-1-oxo-3-phenylmethoxypropan-2-yl]-2-[2-chloro-4-(trifluoromethyl)phenoxy]pyridine-3-carboxamide
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C30H30ClF3N4O4
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0084536
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-[(4-fluorophenyl)methoxy]-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
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C28H27ClF4N4O4
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0046329
N-[(2S)-3-(4-bromophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H26BrCl2N3O2
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0086232
N-[(2S)-1-[(1S,5R)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(4-bromophenyl)-1-oxopropan-2-yl]-1-[4-(trifluoromethoxy)phenyl]cyclopropane-1-carboxamide
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C27H29BrF3N3O3
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0356015
N-[(2S)-1-[(1R,5S)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(4-bromophenyl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C26H28BrCl2N3O2
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0210742
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-[(2-methyl-1,3-oxazol-5-yl)methoxy]-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
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C26H27ClF3N5O5
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0565817
1-(2,4-dichlorophenyl)-N-[(2S)-3-(2,4-dichlorophenyl)-1-[2-(dimethylamino)ethyl-methylamino]-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C24H27Cl4N3O2
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0120672
1-(2,4-dichlorophenyl)-N-[(2S)-1-(4-methylpiperazin-1-yl)-1-oxo-3-phenylmethoxypropan-2-yl]cyclopropane-1-carboxamide
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C25H29Cl2N3O3
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0045196
(2R,3R,4R,5S)-1-[5-(Adamantan-1-ylmethoxy)-pentyl]-2-hydroxymethyl-piperidine-3,4,5-triol
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C22H39NO5
 1
1
IC50 = 16500 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0091328
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-1-(4-methylpiperazin-1-yl)-1-oxo-3-phenylmethoxypropan-2-yl]pyridine-3-carboxamide
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C28H28ClF3N4O4
 1
1 IC50 = 1 nM
CP0236110
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-(2,3-dihydro-1,4-benzodioxin-6-ylmethoxy)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
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C30H30ClF3N4O6
 1
1 IC50 = 1 nM
CP0086232
N-[(2S)-1-[(1S,5R)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(4-bromophenyl)-1-oxopropan-2-yl]-1-[4-(trifluoromethoxy)phenyl]cyclopropane-1-carboxamide
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C27H29BrF3N3O3
 1
1 IC50 = 2 nM
CP0565817
1-(2,4-dichlorophenyl)-N-[(2S)-3-(2,4-dichlorophenyl)-1-[2-(dimethylamino)ethyl-methylamino]-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C24H27Cl4N3O2
 1
1 IC50 = 2 nM
CP0057860
N-[(2S)-1-[(1S,5R)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]-1-[4-(trifluoromethoxy)phenyl]cyclopropane-1-carboxamide
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C27H28Cl2F3N3O3
 1
1 IC50 = 3 nM
CP0356015
N-[(2S)-1-[(1R,5S)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(4-bromophenyl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C26H28BrCl2N3O2
 1
1 IC50 = 3 nM
CP0368789
N-[(2S)-1-[(1R,5S)-3-amino-8-azabicyclo[3.2.1]octan-8-yl]-3-(2,4-dichlorophenyl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C26H27Cl4N3O2
 1
1 IC50 = 4 nM
CP0413929
N-[(2S)-3-(4-bromophenyl)-1-[2-(dimethylamino)ethyl-methylamino]-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H28BrCl2N3O2
 1
1 IC50 = 4 nM
CP0075556
N-[(2R)-1-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-1-oxo-3-phenylmethoxypropan-2-yl]-2-[2-chloro-4-(trifluoromethyl)phenoxy]pyridine-3-carboxamide
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C30H30ClF3N4O4
 1
1 IC50 = 5 nM
CP0084536
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-[(4-fluorophenyl)methoxy]-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
   Show/Hide
C28H27ClF4N4O4
 1
1 IC50 = 7 nM
CP0264143
N-[(2R)-1-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-1-oxo-3-phenylmethoxypropan-2-yl]-2-[2-chloro-4-(trifluoromethyl)phenoxy]pyridine-3-carboxamide
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C30H30ClF3N4O4
 1
1 IC50 = 7 nM
CP0046329
N-[(2S)-3-(4-bromophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H26BrCl2N3O2
 1
1 IC50 = 7 nM
CP0075555
N-[(1R,2S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]nonanamide
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C24H38N2O4
 1
1 IC50 = 9 nM
CP0057863
1-(2,4-dichlorophenyl)-N-[(2S)-3-(1H-indol-3-yl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C26H28Cl2N4O2
 1
1 IC50 = 10 nM
CP0443642
N-[(2S)-3-(4-chlorophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]-1-(2,4-dichlorophenyl)cyclopropane-1-carboxamide
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C24H26Cl3N3O2
 1
1 IC50 = 10 nM
CP0443643
1-(2,4-dichlorophenyl)-N-[(2S)-3-(2,4-dichlorophenyl)-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]cyclopropane-1-carboxamide
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C24H25Cl4N3O2
 1
1 IC50 = 12 nM
CP0070455
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-1-[(3R)-3-(methylamino)pyrrolidin-1-yl]-1-oxo-3-phenylmethoxypropan-2-yl]pyridine-3-carboxamide
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C28H28ClF3N4O4
 1
1 IC50 = 16 nM
CP0191300
N-[(1R,2S)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]octanamide
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C23H36N2O4
 1
1 IC50 = 16 nM
CP0210742
2-[2-chloro-4-(trifluoromethyl)phenoxy]-N-[(2R)-3-[(2-methyl-1,3-oxazol-5-yl)methoxy]-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl]pyridine-3-carboxamide
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C26H27ClF3N5O5
 1
1 IC50 = 20 nM
CP0045196
(2R,3R,4R,5S)-1-[5-(Adamantan-1-ylmethoxy)-pentyl]-2-hydroxymethyl-piperidine-3,4,5-triol
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C22H39NO5
 2
1 IC50 = 90 nM
2 IC50 = 200 nM
CP0120672
1-(2,4-dichlorophenyl)-N-[(2S)-1-(4-methylpiperazin-1-yl)-1-oxo-3-phenylmethoxypropan-2-yl]cyclopropane-1-carboxamide
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C25H29Cl2N3O3
 1
1 IC50 = 90 nM
Clinical Information about the Protein
Target 1 ( Ceramide glucosyltransferase (UGCG) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Type 1 gaucher disease [ICD-11: 5C56.0Y]
2 Fabry disease [ICD-11: 5C56.01]
Approved Drug(s) 1 Approved Drug  1
1 Miglustat Approved
Type 1 gaucher disease
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Venglustat Phase 2
Fabry disease