Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T76685 Target Info
Target Name Cannabinoid receptor 1 (CB1)
Synonyms
Cannabinoid CB1 receptor; CNR; CB-R; CANN6
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Target Type Successful Target
Gene Name CNR1
Biochemical Class GPCR rhodopsin
UniProt ID
CNR1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Pancreatic triacylglycerol lipase (PNLIP) Successful Target
UniProt ID LIPP_HUMAN
Gene Name PNLIP
Synonyms
Pancreatic lipase; PTL; PL
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Representative Drug(s) Orlistat Drug Info IC50 = 0.04 ug.mL-1 [1]
Co-Target Name Cannabinoid receptor 2 (CB2) Successful Target
UniProt ID CNR2_HUMAN
Gene Name CNR2
Synonyms
hCB2; Cannabinoid CB2 receptor; CX5; CB2B; CB2A; CB-2
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Representative Drug(s) SR141716A Drug Info Ki = 1.1 nM Click to Show More [2]
2 Marinol Drug Info EC50 = 1.5 nM [3]
3 NABILONE Drug Info Ki = 1.84 nM [4]
4 SR-147778 Drug Info Ki = 442 nM [9]
Co-Target Name S-mephenytoin 4-hydroxylase (CYP2C9) Successful Target
UniProt ID CP2C9_HUMAN
Gene Name CYP2C9
Synonyms
Cytochrome P450 PB-1; Cytochrome P450 MP-8; Cytochrome P450 MP-4; Cytochrome P450 2C9; Cytochrome P-450MP; Cholesterol 25-hydroxylase; CYPIIC9; CYP2C10; (S)-limonene 7-monooxygenase; (S)-limonene 6-monooxygenase; (R)-limonene 6-monooxygenase
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Representative Drug(s) SR141716A Drug Info IC50 = 5.3 nM [5]
Co-Target Name Dopamine D3 receptor (D3R) Successful Target
UniProt ID DRD3_HUMAN
Gene Name DRD3
Synonyms
D(3) dopamine receptor
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Representative Drug(s) Marinol Drug Info EC50 = 10.2 nM [6]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) SR141716A Drug Info IC50 ~ 20 nM [5]
Co-Target Name Lipoprotein lipase (LPL) Successful Target
UniProt ID LIPL_HUMAN
Gene Name LPL
Synonyms
LIPD
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Representative Drug(s) Orlistat Drug Info IC50 = 66 nM [7]
Co-Target Name Fatty acid synthase (FASN) Successful Target
UniProt ID FAS_HUMAN
Gene Name FASN
Synonyms
Yeast fatty acid synthase; Fatty-acyl-CoA synthase; Fatty acyl-CoA synthetase enzyme; FAS
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Representative Drug(s) Orlistat Drug Info Ki = 280 nM [8]
Co-Target Name Endothelial lipase (LIPG) Clinical trial Target
UniProt ID LIPE_HUMAN
Gene Name LIPG
Synonyms
Endothelial cell-derived lipase; EL; EDL
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Representative Drug(s) Orlistat Drug Info IC50 = 6 nM [7]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) SR141716A Drug Info IC50 ~ 20 nM [5]
Co-Target Name Platelet-activating factor acetylhydrolase (PLA2G7) Clinical trial Target
UniProt ID PAFA_HUMAN
Gene Name PLA2G7
Synonyms
gVIIA-PLA2; PAFAH; PAF acetylhydrolase; PAF 2-acylhydrolase; Lipoprotein-associated phospholipase A2; LDL-associated phospholipase A2; LDL-PLA(2); Group-VIIA phospholipase A2; 2-acetyl-1-alkylglycerophosphocholine esterase; 1-alkyl-2-acetylglycerophosphocholine esterase
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Representative Drug(s) Orlistat Drug Info IC50 = 50 nM [10]
Co-Target Name Diacylglycerol lipase alpha (DAGLA) Patented-recorded Target
UniProt ID DGLA_HUMAN
Gene Name DAGLA
Synonyms
Sn1-specific diacylglycerol lipase alpha; Neural stem cell-derived dendrite regulator; NSDDR; KIAA0659; DGL-alpha; C11orf11
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Representative Drug(s) Orlistat Drug Info IC50 = 1 nM [11]
Co-Target Name Monoacylglycerol lipase ABHD6 (ABHD6) Patented-recorded Target
UniProt ID ABHD6_HUMAN
Gene Name ABHD6
Synonyms
Abhydrolase domain-containing protein 6; 2-arachidonoylglycerol hydrolase
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Representative Drug(s) Orlistat Drug Info IC50 = 13.18 nM [12]
Co-Target Name Diacylglycerol lipase beta (DAGLB) Literature-reported Target
UniProt ID DGLB_HUMAN
Gene Name DAGLB
Synonyms
Sn1-specific diacylglycerol lipase beta; KCCR13L; DGL-beta
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Representative Drug(s) Orlistat Drug Info IC50 = 60 nM [10]
Co-Target Name N-arachidonyl glycine receptor (GPR18) Literature-reported Target
UniProt ID GPR18_HUMAN
Gene Name GPR18
Synonyms
NAGly receptor; GPCRW; G-protein coupled receptor 18
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Representative Drug(s) Marinol Drug Info EC50 = 960 nM [13]
Co-Target Name Hepatic lipase (LIPC) Co-Target
UniProt ID LIPC_HUMAN
Gene Name LIPC
Synonyms
Hepatic triacylglycerol lipase; HL; Lipase member C; Lysophospholipase; Phospholipase A1
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Representative Drug(s) Orlistat Drug Info IC50 = 3 nM [7]
Co-Target Name Cytochrome P450 1A2 (CYP1A2) Co-Target
UniProt ID CP1A2_HUMAN
Gene Name CYP1A2
Synonyms
Cholesterol 25-hydroxylase; Hydroperoxy icosatetraenoate dehydratase; CYPIA2; Cytochrome P(3)450; Cytochrome P450 4; Cytochrome P450-P3
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Representative Drug(s) SR141716A Drug Info IC50 ~ 20 nM [5]
Co-Target Name Phosphatidylserine lipase ABHD16A (ABHD16A) Co-Target
UniProt ID ABHGA_HUMAN
Gene Name ABHD16A
Synonyms
Alpha/beta hydrolase domain-containing protein 16A; Abhydrolase domain-containing protein 16A; HLA-B-associated transcript 5; hBAT5; Monoacylglycerol lipase ABHD16A; Protein G5
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Representative Drug(s) Orlistat Drug Info IC50 = 30 nM [10]
Co-Target Name Monoacylglycerol lipase ABHD12 (ABHD12) Co-Target
UniProt ID ABD12_HUMAN
Gene Name ABHD12
Synonyms
Lysophosphatidylserine lipase ABHD12; 2-arachidonoylglycerol hydrolase ABHD12; Abhydrolase domain-containing protein 12; hABHD12; Oxidized phosphatidylserine lipase ABHD12
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Representative Drug(s) Orlistat Drug Info IC50 = 80 nM [10]
References  Top
REF 1 Biologically active triterpenoid saponins from Acanthopanax senticosus. J Nat Prod. 2006 Nov;69(11):1577-81.
REF 2 Ultrapure ajulemic acid has improved CB2 selectivity with reduced CB1 activity. Bioorg Med Chem. 2014 Jul 1;22(13):3245-51.
REF 3 Novel benzimidazole derivatives as selective CB2 agonists. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3695-700.
REF 4 Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. J Med Chem. 2013 Nov 14;56(21):8224-56.
REF 5 Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist. Bioorg Med Chem. 2010 Sep 1;18(17):6377-88.
REF 6 Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase. J Med Chem. 2017 Mar 23;60(6):2287-304.
REF 7 Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase. ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268.
REF 8 The lipogenesis pathway as a cancer target. J Med Chem. 2011 Aug 25;54(16):5615-38.
REF 9 The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. J Med Chem. 2005 Aug 11;48(16):5059-87.
REF 10 Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5838-41.
REF 11 Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase. Bioorg Med Chem. 2016 Apr 1;24(7):1455-68.
REF 12 Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors. Bioorg Med Chem. 2015 Oct 1;23(19):6335-45.
REF 13 Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55. Medchemcomm. 2014;5:632-49.

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