Target Information
| Target General Information | Top | |||||
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| Target ID |
T76685
(Former ID: TTDS00334)
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| Target Name |
Cannabinoid receptor 1 (CB1)
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| Synonyms |
Cannabinoid CB1 receptor; CNR; CB-R; CANN6
Click to Show/Hide
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| Gene Name |
CNR1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Anorexia nervosa [ICD-11: 6B80] | |||||
| 2 | Insomnia [ICD-11: 7A00-7A0Z] | |||||
| 3 | Obesity [ICD-11: 5B80-5B81] | |||||
| Function |
Mediates many cannabinoid-induced effects, acting, among others, on food intake, memory loss, gastrointestinal motility, catalepsy, ambulatory activity, anxiety, chronic pain. Signaling typically involves reduction in cyclic AMP. In the hypothalamus, may have a dual effect on mitochondrial respiration depending upon the agonist dose and possibly upon the cell type. Increases respiration at low doses, while decreases respiration at high doses. At high doses, CNR1 signal transduction involves G-protein alpha-i protein activation and subsequent inhibition of mitochondrial soluble adenylate cyclase, decrease in cyclic AMP concentration, inhibition of protein kinase A (PKA)-dependent phosphorylation of specific subunits of the mitochondrial electron transport system, including NDUFS2. In the hypothalamus, inhibits leptin-induced reactive oxygen species (ROS) formation and mediates cannabinoid-induced increase in SREBF1 and FASN gene expression. In response to cannabinoids, drives the release of orexigenic beta-endorphin, but not that of melanocyte-stimulating hormone alpha/alpha-MSH, from hypothalamic POMC neurons, hence promoting food intake. In the hippocampus, regulates cellular respiration and energy production in response to cannabinoids. Involved in cannabinoid-dependent depolarization-induced suppression of inhibition (DSI), a process in which depolarization of CA1 postsynaptic pyramidal neurons mobilizes eCBs, which retrogradely activate presynaptic CB1 receptors, transiently decreasing GABAergic inhibitory neurotransmission. Also reduces excitatory synaptic transmission. In superior cervical ganglions and cerebral vascular smooth muscle cells, inhibits voltage-gated Ca(2+) channels in a constitutive, as well as agonist-dependent manner. In cerebral vascular smooth muscle cells, cannabinoid-induced inhibition of voltage-gated Ca(2+) channels leads to vasodilation and decreased vascular tone. Induces leptin production in adipocytes and reduces LRP2-mediated leptin clearance in the kidney, hence participating in hyperleptinemia. In adipose tissue, CNR1 signaling leads to increased expression of SREBF1, ACACA and FASN genes. In the liver, activation by endocannabinoids leads to increased de novo lipogenesis and reduced fatty acid catabolism, associated with increased expression of SREBF1/SREBP-1, GCK, ACACA, ACACB and FASN genes. May also affect de novo cholesterol synthesis and HDL-cholesteryl ether uptake. Peripherally modulates energy metabolism. In high carbohydrate diet-induced obesity, may decrease the expression of mitochondrial dihydrolipoyl dehydrogenase/DLD in striated muscles, as well as that of selected glucose/ pyruvate metabolic enzymes, hence affecting energy expenditure through mitochondrial metabolism. In response to cannabinoid anandamide, elicits a proinflammatory response in macrophages, which involves NLRP3 inflammasome activation and IL1B and IL18 secretion. In macrophages infiltrating pancreatic islets, this process may participate in the progression of type-2 diabetes and associated loss of pancreatic beta-cells. G-protein coupled receptor for endogenous cannabinoids (eCBs), including N-arachidonoylethanolamide (also called anandamide or AEA) and 2-arachidonoylglycerol (2-AG), as well as phytocannabinoids, such as delta(9)-tetrahydrocannabinol (THC).
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T17E49 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Marinol | Drug Info | Approved | Anorexia nervosa cachexia | [2] | |
| 2 | NABILONE | Drug Info | Approved | Insomnia | [3] | |
| 3 | Orlistat | Drug Info | Approved | Obesity | [3], [4], [5], [6] | |
| 4 | SR141716A | Drug Info | Approved | Obesity | [3], [7] | |
| Clinical Trial Drug(s) | [+] 10 Clinical Trial Drugs | + | ||||
| 1 | Tebipenem | Drug Info | Phase 3 | Urinary tract infection | [8] | |
| 2 | AEF0117 | Drug Info | Phase 2 | Marijuana use disorder | [9] | |
| 3 | Conatumumab | Drug Info | Phase 2 | Colorectal cancer | [10] | |
| 4 | GW-42004 | Drug Info | Phase 2 | Lipid metabolism disorder | [11] | |
| 5 | Nimacimab | Drug Info | Phase 2 | Diabetic nephropathy | [12] | |
| 6 | SR-147778 | Drug Info | Phase 2 | Obesity | [13] | |
| 7 | GFB-024 | Drug Info | Phase 1 | Diabetic nephropathy | [14] | |
| 8 | TM38837 | Drug Info | Phase 1 | Metabolic disorder | [15], [16] | |
| 9 | V-24343 | Drug Info | Phase 1 | Type-2 diabetes | [17] | |
| 10 | ZY01 | Drug Info | Phase 1 | Diabetic complication | [18] | |
| Patented Agent(s) | [+] 153 Patented Agents | + | ||||
| 1 | 1,2,3-triazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 2 | 1,2,3-triazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 3 | 1,2,4,5-tetra-substituted imidazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 4 | 1,2,4,5-tetra-substituted imidazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 5 | 1,2,4-tri-substituted imidazoline derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 6 | 1,2,4-triazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 7 | 1,2,4-triazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 8 | 1,5-diphenylpyrrolidin-2-one derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 9 | 1,5-diphenylpyrrolidin-2-one derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 10 | 4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 11 | Amide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 12 | Aminoazetidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 13 | Aminoazetidine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 14 | Aminoazetidine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 15 | Aminoazetidine derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 16 | Aminoazetidine derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 17 | Aminoazetidine derivative 7 | Drug Info | Patented | Obesity | [19] | |
| 18 | Aminoazetidine derivative 8 | Drug Info | Patented | Obesity | [19] | |
| 19 | Aminoazetidine derivative 9 | Drug Info | Patented | Obesity | [19] | |
| 20 | Azetidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 21 | Azetidine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 22 | Azetidine derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 23 | Azetidine-1-carboxamide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 24 | Azetidine-1-carboxamide derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 25 | Azetidine-1-carboxamide derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 26 | Benzimidazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 27 | Benzimidazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 28 | Carboxamide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 29 | Diaryl morpholine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 30 | Diaryl piperazine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 31 | Diaryl piperazine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 32 | Diphenyl purine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 33 | Diphenyl purine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 34 | Diphenyl purine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 35 | Diphenyl purine derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 36 | Diphenyl purine derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 37 | Furopyridine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 38 | Furopyridine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 39 | Heterocyclic-substituted 3-alkyl azetidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 40 | Heterocyclic-substituted 3-alkyl azetidine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 41 | Heterocyclic-substituted 3-alkyl azetidine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 42 | Hydrazide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 43 | Imidazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 44 | Imidazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 45 | Imidazole derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 46 | Imidazole derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 47 | Imidazole derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 48 | Imidazole derivative 6 | Drug Info | Patented | Obesity | [19] | |
| 49 | Imidazole derivative 7 | Drug Info | Patented | Obesity | [19] | |
| 50 | Imidazolidine-2,4-dione derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 51 | Imidazolidine-2,4-dione derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 52 | N,N-methylenebis-2-phenylacetamide and benzenesulfonamide derivative 2 | Drug Info | Patented | Osteoporosis | [20] | |
| 53 | N,N-methylenebis-2-phenylacetamide and benzenesulfonamide derivative 3 | Drug Info | Patented | Osteoporosis | [20] | |
| 54 | N-(arylalkyl)-1H-indole-2-sulfonic acid amide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 55 | N-(arylalkyl)-1H-indole-2-sulfonic acid amide derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 56 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 57 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 58 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 59 | Piperazine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 60 | Piperazine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 61 | PMID26161824-Compound-68 | Drug Info | Patented | Obesity | [19] | |
| 62 | PMID26161824-Compound-69 | Drug Info | Patented | Obesity | [19] | |
| 63 | PMID27215781-Compound-37 | Drug Info | Patented | Prostate cancer | [20] | |
| 64 | Purine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 65 | Purine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 66 | Purine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 67 | Pyrano[2,3-b]pyridine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 68 | Pyrano[2,3-b]pyridine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 69 | Pyrazole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 70 | Pyrazole derivative 11 | Drug Info | Patented | Obesity | [19] | |
| 71 | Pyrazole derivative 12 | Drug Info | Patented | Obesity | [19] | |
| 72 | Pyrazole derivative 13 | Drug Info | Patented | Obesity | [19] | |
| 73 | Pyrazole derivative 14 | Drug Info | Patented | Obesity | [19] | |
| 74 | Pyrazole derivative 15 | Drug Info | Patented | Obesity | [19] | |
| 75 | Pyrazole derivative 16 | Drug Info | Patented | Obesity | [19] | |
| 76 | Pyrazole derivative 17 | Drug Info | Patented | Obesity | [19] | |
| 77 | Pyrazole derivative 18 | Drug Info | Patented | Obesity | [19] | |
| 78 | Pyrazole derivative 19 | Drug Info | Patented | Obesity | [19] | |
| 79 | Pyrazole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 80 | Pyrazole derivative 20 | Drug Info | Patented | Obesity | [19] | |
| 81 | Pyrazole derivative 21 | Drug Info | Patented | Obesity | [19] | |
| 82 | Pyrazole derivative 22 | Drug Info | Patented | Obesity | [19] | |
| 83 | Pyrazole derivative 23 | Drug Info | Patented | Obesity | [19] | |
| 84 | Pyrazole derivative 24 | Drug Info | Patented | Obesity | [19] | |
| 85 | Pyrazole derivative 25 | Drug Info | Patented | Obesity | [19] | |
| 86 | Pyrazole derivative 26 | Drug Info | Patented | Obesity | [19] | |
| 87 | Pyrazole derivative 27 | Drug Info | Patented | Obesity | [19] | |
| 88 | Pyrazole derivative 28 | Drug Info | Patented | Obesity | [19] | |
| 89 | Pyrazole derivative 29 | Drug Info | Patented | Obesity | [19] | |
| 90 | Pyrazole derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 91 | Pyrazole derivative 30 | Drug Info | Patented | Obesity | [19] | |
| 92 | Pyrazole derivative 31 | Drug Info | Patented | Obesity | [19] | |
| 93 | Pyrazole derivative 32 | Drug Info | Patented | Obesity | [19] | |
| 94 | Pyrazole derivative 33 | Drug Info | Patented | Obesity | [19] | |
| 95 | Pyrazole derivative 34 | Drug Info | Patented | Obesity | [19] | |
| 96 | Pyrazole derivative 35 | Drug Info | Patented | Obesity | [19] | |
| 97 | Pyrazole derivative 36 | Drug Info | Patented | Obesity | [19] | |
| 98 | Pyrazole derivative 37 | Drug Info | Patented | Obesity | [19] | |
| 99 | Pyrazole derivative 38 | Drug Info | Patented | Obesity | [19] | |
| 100 | Pyrazole derivative 39 | Drug Info | Patented | Obesity | [19] | |
| 101 | Pyrazole derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 102 | Pyrazole derivative 40 | Drug Info | Patented | Obesity | [19] | |
| 103 | Pyrazole derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 104 | Pyrazole derivative 53 | Drug Info | Patented | Obesity | [19] | |
| 105 | Pyrazole derivative 54 | Drug Info | Patented | Obesity | [19] | |
| 106 | Pyrazole derivative 57 | Drug Info | Patented | Obesity | [19] | |
| 107 | Pyrazole derivative 58 | Drug Info | Patented | Obesity | [19] | |
| 108 | Pyrazole derivative 59 | Drug Info | Patented | Obesity | [19] | |
| 109 | Pyrazole derivative 6 | Drug Info | Patented | Obesity | [19] | |
| 110 | Pyrazole derivative 60 | Drug Info | Patented | Obesity | [19] | |
| 111 | Pyrazole derivative 7 | Drug Info | Patented | Obesity | [19] | |
| 112 | Pyrazole derivative 8 | Drug Info | Patented | Obesity | [19] | |
| 113 | Pyrazoline derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 114 | Pyrazoline derivative 10 | Drug Info | Patented | Obesity | [19] | |
| 115 | Pyrazoline derivative 11 | Drug Info | Patented | Obesity | [19] | |
| 116 | Pyrazoline derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 117 | Pyrazoline derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 118 | Pyrazoline derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 119 | Pyrazoline derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 120 | Pyrazolo[1,5-a]pyrimidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 121 | Pyrazolo[1,5-a]pyrimidine derivative 10 | Drug Info | Patented | Obesity | [19] | |
| 122 | Pyrazolo[1,5-a]pyrimidine derivative 11 | Drug Info | Patented | Obesity | [19] | |
| 123 | Pyrazolo[1,5-a]pyrimidine derivative 12 | Drug Info | Patented | Obesity | [19] | |
| 124 | Pyrazolo[1,5-a]pyrimidine derivative 13 | Drug Info | Patented | Obesity | [19] | |
| 125 | Pyrazolo[1,5-a]pyrimidine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 126 | Pyrazolo[1,5-a]pyrimidine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 127 | Pyrazolo[1,5-a]pyrimidine derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 128 | Pyrazolo[1,5-a]pyrimidine derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 129 | Pyrazolo[1,5-a]pyrimidine derivative 6 | Drug Info | Patented | Obesity | [19] | |
| 130 | Pyrazolo[1,5-a]pyrimidine derivative 7 | Drug Info | Patented | Obesity | [19] | |
| 131 | Pyrazolo[1,5-a]pyrimidine derivative 8 | Drug Info | Patented | Obesity | [19] | |
| 132 | Pyrazolo[1,5-a]pyrimidine derivative 9 | Drug Info | Patented | Obesity | [19] | |
| 133 | Pyridotriazolopyrimidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 134 | Pyridotriazolopyrimidine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 135 | Pyridotriazolopyrimidine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 136 | Pyrido[2,3-d]pyrimidine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 137 | Pyrido[2,3-d]pyrimidine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 138 | Pyrrole derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 139 | Pyrrole derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 140 | Pyrrole derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 141 | Pyrrole derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 142 | Pyrrole derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 143 | Pyrrole derivative 6 | Drug Info | Patented | Obesity | [19] | |
| 144 | Sulfonamide derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 145 | Sulfonylated piperazine derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 146 | Sulfonylated piperazine derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 147 | Sulfonylated piperazine derivative 3 | Drug Info | Patented | Obesity | [19] | |
| 148 | Sulfonylated piperazine derivative 4 | Drug Info | Patented | Obesity | [19] | |
| 149 | Sulfonylated piperazine derivative 5 | Drug Info | Patented | Obesity | [19] | |
| 150 | Tetra-hydro-1H-1,2,6-triazaazulene derivative 1 | Drug Info | Patented | Obesity | [19] | |
| 151 | Tetra-hydro-1H-1,2,6-triazaazulene derivative 2 | Drug Info | Patented | Obesity | [19] | |
| 152 | Tricyclic phytocannabinoid derivative 1 | Drug Info | Patented | Neuropathic pain | [20] | |
| 153 | Tricyclic phytocannabinoid derivative 2 | Drug Info | Patented | Neuropathic pain | [20] | |
| Discontinued Drug(s) | [+] 13 Discontinued Drugs | + | ||||
| 1 | CP-945598 | Drug Info | Discontinued in Phase 3 | Obesity | [21] | |
| 2 | Taranabant | Drug Info | Discontinued in Phase 3 | Obesity | [22] | |
| 3 | AVE1625 | Drug Info | Discontinued in Phase 2 | Psychotic disorder | [23] | |
| 4 | AZD2207 | Drug Info | Discontinued in Phase 2 | Obesity | [24] | |
| 5 | KDS-2000 | Drug Info | Discontinued in Phase 2 | Postherpetic neuralgia | [25] | |
| 6 | KN-38-7271 | Drug Info | Discontinued in Phase 2 | Ischemia | [26] | |
| 7 | SLV319 | Drug Info | Discontinued in Phase 2 | Obesity | [27] | |
| 8 | AZD1175 | Drug Info | Discontinued in Phase 1 | Obesity | [28] | |
| 9 | AZD1704 | Drug Info | Discontinued in Phase 1 | Pain | [29] | |
| 10 | CBD cannabis derivative | Drug Info | Discontinued in Phase 1 | Schizophrenia | [30] | |
| 11 | PF-514273 | Drug Info | Discontinued in Phase 1 | Obesity | [31] | |
| 12 | TAK-937 | Drug Info | Discontinued in Phase 1 | Cerebrovascular ischaemia | [32] | |
| 13 | Dianicline+rimonabant | Drug Info | Terminated | Tobacco dependence | [34] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | CB1 antagonist, Bayer | Drug Info | Preclinical | Obesity | [21] | |
| 2 | JD-5037 | Drug Info | Preclinical | Diabetic complication | [33] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Agonist | [+] 23 Agonist drugs | + | ||||
| 1 | Marinol | Drug Info | [1], [35] | |||
| 2 | Conatumumab | Drug Info | [42] | |||
| 3 | GFB-024 | Drug Info | [14] | |||
| 4 | Carbazole-3-carboxamide analog 1 | Drug Info | [20] | |||
| 5 | Cyano(dimethyl)methyl isoxazoles and [1,3,4]-thiadiazoles derivative 1 | Drug Info | [20] | |||
| 6 | Cyano(dimethyl)methyl isoxazoles and [1,3,4]-thiadiazoles derivative 2 | Drug Info | [20] | |||
| 7 | PMID27215781-Compound-1 | Drug Info | [20] | |||
| 8 | PMID27215781-Compound-2 | Drug Info | [20] | |||
| 9 | KDS-2000 | Drug Info | [25] | |||
| 10 | JD-5037 | Drug Info | [33] | |||
| 11 | Dianicline+rimonabant | Drug Info | [54] | |||
| 12 | ACEA | Drug Info | [72], [73] | |||
| 13 | Anandamide | Drug Info | [79] | |||
| 14 | arachidonylcyclopropylamide | Drug Info | [72] | |||
| 15 | AZ-599 | Drug Info | [80] | |||
| 16 | cannabinol | Drug Info | [81] | |||
| 17 | Dibenzothiazepines | Drug Info | [80] | |||
| 18 | HU210 | Drug Info | [39] | |||
| 19 | MK-5596 | Drug Info | [80] | |||
| 20 | O-1812 | Drug Info | [98] | |||
| 21 | [3H]CP55940 | Drug Info | [105], [55] | |||
| 22 | [3H]HU-243 | Drug Info | [106] | |||
| 23 | [3H]WIN55212-2 | Drug Info | [107] | |||
| Inhibitor | [+] 165 Inhibitor drugs | + | ||||
| 1 | NABILONE | Drug Info | [36] | |||
| 2 | Orlistat | Drug Info | [37] | |||
| 3 | WIN-55212-2 | Drug Info | [55] | |||
| 4 | (1R,2R)-N-Arachidonoylcyclopropanolamide | Drug Info | [56] | |||
| 5 | (1R,2S)-N-Arachidonoylcyclopropanolamide | Drug Info | [56] | |||
| 6 | (1R,2S)-N-Oleoylcyclopropanolamide | Drug Info | [56] | |||
| 7 | (1S,2S)-N-Arachidonoylcyclopropanolamide | Drug Info | [56] | |||
| 8 | (1S,2S)-N-Oleoylcyclopropanolamide | Drug Info | [56] | |||
| 9 | (2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 10 | (2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 11 | (2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 12 | (4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone | Drug Info | [58] | |||
| 13 | (E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide | Drug Info | [59] | |||
| 14 | (E)-N-(4-methoxyphenethyl)undec-2-enamide | Drug Info | [59] | |||
| 15 | (E)-N-(4-methoxyphenyl)undec-2-enamide | Drug Info | [59] | |||
| 16 | 1,3,5-triphenylimidazolidine-2,4-dione | Drug Info | [60] | |||
| 17 | 1,3,5-tris(4-chlorophenyl)imidazolidine-2,4-dione | Drug Info | [60] | |||
| 18 | 1,4-dihydroindeno[1,2-c]-pyrazole | Drug Info | [61] | |||
| 19 | 1,5-bis(4-chlorophenyl)-1H-1,2,3-triazole | Drug Info | [62] | |||
| 20 | 1-(2-morpholinoethyl)-1H-indol-3-yl acetate | Drug Info | [63] | |||
| 21 | 1-(4-CHLOROPHENYL)-2-(2,4-DICHLOROPHENYL)-5-(METHYLSULFINYL)-N-(PIPERIDIN-1-YL)-1H-IMIDAZOLE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | [64] | |||
| 22 | 1-(bis(4-bromophenyl)methyl)-3-phenylurea | Drug Info | [65] | |||
| 23 | 1-(bis(4-chlorophenyl)methyl)-3-phenylurea | Drug Info | [65] | |||
| 24 | 1-[bis(4-bromophenyl)methyl]-3-phenylthiourea | Drug Info | [65] | |||
| 25 | 1-[bis(4-chlorophenyl)methyl]-3-(4-chlorophenyl)- | Drug Info | [65] | |||
| 26 | 1-[bis(4-chlorophenyl)methyl]-3-phenylthiourea | Drug Info | [65] | |||
| 27 | 1-[bis(4-iodophenyl)methyl]-3-(4-bromophenyl)urea | Drug Info | [65] | |||
| 28 | 2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | [66] | |||
| 29 | 2-Benzylbenzo[f]chromen-3-one | Drug Info | [55] | |||
| 30 | 3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | [66] | |||
| 31 | 3,4-diarylpyrazoline derivative | Drug Info | [67] | |||
| 32 | 3-Benzyl-5-isopropyl-8-methylchromen-2-one | Drug Info | [55] | |||
| 33 | 3-Benzyl-5-methoxy-7-methylchromen-2-one | Drug Info | [55] | |||
| 34 | 3-Benzyl-5-methoxychromen-2-one | Drug Info | [55] | |||
| 35 | 4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | [66] | |||
| 36 | 4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol | Drug Info | [66] | |||
| 37 | 4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol | Drug Info | [66] | |||
| 38 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [68] | |||
| 39 | 4-benzhydryl-N-butylpiperazine-1-carboxamide | Drug Info | [58] | |||
| 40 | 4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide | Drug Info | [58] | |||
| 41 | 4-cyanophenyl ethyl dodecylphosphonate | Drug Info | [69] | |||
| 42 | 5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol | Drug Info | [66] | |||
| 43 | 5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole | Drug Info | [70] | |||
| 44 | 5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one | Drug Info | [55] | |||
| 45 | 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 46 | 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 47 | 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 48 | 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 49 | A-796260 | Drug Info | [71] | |||
| 50 | AM-1241 | Drug Info | [71] | |||
| 51 | AM-1710 | Drug Info | [74] | |||
| 52 | AM-1714 | Drug Info | [74] | |||
| 53 | AM-1715 | Drug Info | [74] | |||
| 54 | AM-281 | Drug Info | [55] | |||
| 55 | AM-404 | Drug Info | [75] | |||
| 56 | AM-411 | Drug Info | [76] | |||
| 57 | AM-4768 | Drug Info | [74] | |||
| 58 | AM-630 | Drug Info | [77] | |||
| 59 | Chlorphrifos oxon | Drug Info | [69] | |||
| 60 | Cis-N-oleoylcyclopropanolamide | Drug Info | [56] | |||
| 61 | CP-4497 | Drug Info | [82] | |||
| 62 | DELTA 8-TETRAHYDROCANNOBINOL | Drug Info | [83] | |||
| 63 | Dodecane-1-sulfonyl fluoride | Drug Info | [69] | |||
| 64 | Isopropyl 4-nitrophenyl dodecylphosphonate | Drug Info | [69] | |||
| 65 | Isopropyl dodecylfluorophosphonate | Drug Info | [84] | |||
| 66 | JWH-120 | Drug Info | [85] | |||
| 67 | JWH-133 | Drug Info | [86] | |||
| 68 | JWH-145 | Drug Info | [87] | |||
| 69 | JWH-146 | Drug Info | [87] | |||
| 70 | JWH-147 | Drug Info | [87] | |||
| 71 | JWH-150 | Drug Info | [87] | |||
| 72 | JWH-156 | Drug Info | [87] | |||
| 73 | JWH-229 | Drug Info | [85] | |||
| 74 | JWH-243 | Drug Info | [87] | |||
| 75 | JWH-244 | Drug Info | [87] | |||
| 76 | JWH-245 | Drug Info | [87] | |||
| 77 | JWH-246 | Drug Info | [87] | |||
| 78 | JWH-268 | Drug Info | [85] | |||
| 79 | JWH-292 | Drug Info | [87] | |||
| 80 | JWH-293 | Drug Info | [87] | |||
| 81 | JWH-297 | Drug Info | [88] | |||
| 82 | JWH-307 | Drug Info | [87] | |||
| 83 | JWH-308 | Drug Info | [87] | |||
| 84 | JWH-309 | Drug Info | [87] | |||
| 85 | JWH-324 | Drug Info | [82] | |||
| 86 | JWH-325 | Drug Info | [88] | |||
| 87 | JWH-337 | Drug Info | [88] | |||
| 88 | JWH-342 | Drug Info | [88] | |||
| 89 | JWH-344 | Drug Info | [88] | |||
| 90 | JWH-345 | Drug Info | [88] | |||
| 91 | JWH-346 | Drug Info | [87] | |||
| 92 | JWH-347 | Drug Info | [87] | |||
| 93 | JWH-348 | Drug Info | [87] | |||
| 94 | JWH-363 | Drug Info | [87] | |||
| 95 | JWH-364 | Drug Info | [87] | |||
| 96 | JWH-365 | Drug Info | [87] | |||
| 97 | JWH-366 | Drug Info | [87] | |||
| 98 | JWH-367 | Drug Info | [87] | |||
| 99 | JWH-368 | Drug Info | [87] | |||
| 100 | JWH-369 | Drug Info | [87] | |||
| 101 | JWH-370 | Drug Info | [87] | |||
| 102 | JWH-371 | Drug Info | [87] | |||
| 103 | JWH-372 | Drug Info | [87] | |||
| 104 | JWH-373 | Drug Info | [87] | |||
| 105 | JWH-385 | Drug Info | [88] | |||
| 106 | JWH-392 | Drug Info | [88] | |||
| 107 | JWH-401 | Drug Info | [88] | |||
| 108 | JWH-402 | Drug Info | [88] | |||
| 109 | JWH-403 | Drug Info | [88] | |||
| 110 | JWH-404 | Drug Info | [88] | |||
| 111 | JWH-405 | Drug Info | [88] | |||
| 112 | JWH-406 | Drug Info | [88] | |||
| 113 | JWH-407 | Drug Info | [88] | |||
| 114 | JWH-440 | Drug Info | [82] | |||
| 115 | JWH-442 | Drug Info | [82] | |||
| 116 | KM-233 | Drug Info | [89] | |||
| 117 | KM-233-M | Drug Info | [89] | |||
| 118 | Methyl icosylphosphonofluoridate | Drug Info | [69] | |||
| 119 | N-(1-adamantyl)-N'-propylsulfamide | Drug Info | [92] | |||
| 120 | N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide | Drug Info | [93] | |||
| 121 | N-(2,4-dimethoxyphenethyl)docos-13-enamide | Drug Info | [59] | |||
| 122 | N-(2,4-dimethoxyphenethyl)oleamide | Drug Info | [59] | |||
| 123 | N-(2-adamantyl)-N'-propylsulfamide | Drug Info | [92] | |||
| 124 | N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide | Drug Info | [77] | |||
| 125 | N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide | Drug Info | [94] | |||
| 126 | N-(3,3-Diphenyl)propyl-2-phenylacetamide | Drug Info | [94] | |||
| 127 | N-(3,5-dimethoxyphenethyl)docos-13-enamide | Drug Info | [59] | |||
| 128 | N-(3,5-dimethoxyphenethyl)oleamide | Drug Info | [59] | |||
| 129 | N-(3-Phenyl)propyl-2,2-diphenylacetamide | Drug Info | [94] | |||
| 130 | N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) | Drug Info | [94] | |||
| 131 | N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide | Drug Info | [93] | |||
| 132 | N-(4-methoxybenzyl)oleamide | Drug Info | [59] | |||
| 133 | N-(4-methoxyphenethyl)oleamide | Drug Info | [59] | |||
| 134 | N-(4-methoxyphenyl)oleamide | Drug Info | [59] | |||
| 135 | N-(4-morpholinophenyl)docos-13-enamide | Drug Info | [59] | |||
| 136 | N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 137 | N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 138 | N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 139 | N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 140 | N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) | Drug Info | [57] | |||
| 141 | N-(cis-9-cis-12-octadecadienyl)sulfamide | Drug Info | [92] | |||
| 142 | N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine | Drug Info | [95] | |||
| 143 | N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine | Drug Info | [95] | |||
| 144 | N-ethyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | [96] | |||
| 145 | N-isopentyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | [96] | |||
| 146 | N-isopropyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | [96] | |||
| 147 | N-methyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | [96] | |||
| 148 | N-octadecyl-N'-propylsulfamide | Drug Info | [92] | |||
| 149 | N-oleoylethanolamide | Drug Info | [56] | |||
| 150 | N-phenyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | [96] | |||
| 151 | N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) | Drug Info | [97] | |||
| 152 | NAPHTHYRIDINONE | Drug Info | [57] | |||
| 153 | O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine | Drug Info | [95] | |||
| 154 | Octane-1-sulfonyl fluoride | Drug Info | [69] | |||
| 155 | PARAOXON | Drug Info | [69] | |||
| 156 | PRAVADOLINE | Drug Info | [100] | |||
| 157 | Rac-cis-N-arachidonoylcyclopropanolamide | Drug Info | [56] | |||
| 158 | Rac-trans-N-oleoylcyclopropanolamide | Drug Info | [56] | |||
| 159 | SCH-356036 | Drug Info | [101] | |||
| 160 | SEMIPLENAMIDE A | Drug Info | [102] | |||
| 161 | SEMIPLENAMIDE B | Drug Info | [102] | |||
| 162 | Semiplenamide G | Drug Info | [102] | |||
| 163 | VER-156084 | Drug Info | [103] | |||
| 164 | VER-156085 | Drug Info | [103] | |||
| 165 | {[(9Z)-octadec-9-en-1-yl]sulfamoyl}amine | Drug Info | [92] | |||
| Antagonist | [+] 171 Antagonist drugs | + | ||||
| 1 | SR141716A | Drug Info | [38], [39], [40] | |||
| 2 | Tebipenem | Drug Info | [21] | |||
| 3 | AEF0117 | Drug Info | [41] | |||
| 4 | Nimacimab | Drug Info | [44] | |||
| 5 | TM38837 | Drug Info | [16] | |||
| 6 | V-24343 | Drug Info | [46] | |||
| 7 | ZY01 | Drug Info | [18] | |||
| 8 | 1,2,3-triazole derivative 1 | Drug Info | [19] | |||
| 9 | 1,2,3-triazole derivative 2 | Drug Info | [19] | |||
| 10 | 1,2,4,5-tetra-substituted imidazole derivative 1 | Drug Info | [19] | |||
| 11 | 1,2,4,5-tetra-substituted imidazole derivative 2 | Drug Info | [19] | |||
| 12 | 1,2,4-tri-substituted imidazoline derivative 1 | Drug Info | [19] | |||
| 13 | 1,2,4-triazole derivative 1 | Drug Info | [19] | |||
| 14 | 1,2,4-triazole derivative 2 | Drug Info | [19] | |||
| 15 | 1,5-diphenylpyrrolidin-2-one derivative 1 | Drug Info | [19] | |||
| 16 | 1,5-diphenylpyrrolidin-2-one derivative 2 | Drug Info | [19] | |||
| 17 | 4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide derivative 1 | Drug Info | [19] | |||
| 18 | Amide derivative 1 | Drug Info | [19] | |||
| 19 | Aminoazetidine derivative 1 | Drug Info | [19] | |||
| 20 | Aminoazetidine derivative 2 | Drug Info | [19] | |||
| 21 | Aminoazetidine derivative 3 | Drug Info | [19] | |||
| 22 | Aminoazetidine derivative 4 | Drug Info | [19] | |||
| 23 | Aminoazetidine derivative 5 | Drug Info | [19] | |||
| 24 | Aminoazetidine derivative 7 | Drug Info | [19] | |||
| 25 | Aminoazetidine derivative 8 | Drug Info | [19] | |||
| 26 | Aminoazetidine derivative 9 | Drug Info | [19] | |||
| 27 | Azetidine derivative 1 | Drug Info | [19] | |||
| 28 | Azetidine derivative 3 | Drug Info | [19] | |||
| 29 | Azetidine derivative 4 | Drug Info | [19] | |||
| 30 | Azetidine-1-carboxamide derivative 1 | Drug Info | [19] | |||
| 31 | Azetidine-1-carboxamide derivative 2 | Drug Info | [19] | |||
| 32 | Azetidine-1-carboxamide derivative 3 | Drug Info | [19] | |||
| 33 | Benzimidazole derivative 1 | Drug Info | [19] | |||
| 34 | Benzimidazole derivative 2 | Drug Info | [19] | |||
| 35 | Carboxamide derivative 1 | Drug Info | [19] | |||
| 36 | Diaryl morpholine derivative 1 | Drug Info | [19] | |||
| 37 | Diaryl piperazine derivative 1 | Drug Info | [19] | |||
| 38 | Diaryl piperazine derivative 2 | Drug Info | [19] | |||
| 39 | Diphenyl purine derivative 1 | Drug Info | [19] | |||
| 40 | Diphenyl purine derivative 2 | Drug Info | [19] | |||
| 41 | Diphenyl purine derivative 3 | Drug Info | [19] | |||
| 42 | Diphenyl purine derivative 4 | Drug Info | [19] | |||
| 43 | Diphenyl purine derivative 5 | Drug Info | [19] | |||
| 44 | Furopyridine derivative 1 | Drug Info | [19] | |||
| 45 | Furopyridine derivative 2 | Drug Info | [19] | |||
| 46 | Heterocyclic-substituted 3-alkyl azetidine derivative 1 | Drug Info | [19] | |||
| 47 | Heterocyclic-substituted 3-alkyl azetidine derivative 2 | Drug Info | [19] | |||
| 48 | Heterocyclic-substituted 3-alkyl azetidine derivative 3 | Drug Info | [19] | |||
| 49 | Hydrazide derivative 1 | Drug Info | [19] | |||
| 50 | Imidazole derivative 1 | Drug Info | [19] | |||
| 51 | Imidazole derivative 2 | Drug Info | [19] | |||
| 52 | Imidazole derivative 3 | Drug Info | [19] | |||
| 53 | Imidazole derivative 4 | Drug Info | [19] | |||
| 54 | Imidazole derivative 5 | Drug Info | [19] | |||
| 55 | Imidazole derivative 6 | Drug Info | [19] | |||
| 56 | Imidazole derivative 7 | Drug Info | [19] | |||
| 57 | Imidazolidine-2,4-dione derivative 1 | Drug Info | [19] | |||
| 58 | Imidazolidine-2,4-dione derivative 2 | Drug Info | [19] | |||
| 59 | N-(arylalkyl)-1H-indole-2-sulfonic acid amide derivative 1 | Drug Info | [19] | |||
| 60 | N-(arylalkyl)-1H-indole-2-sulfonic acid amide derivative 2 | Drug Info | [19] | |||
| 61 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 1 | Drug Info | [19] | |||
| 62 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 2 | Drug Info | [19] | |||
| 63 | N-phenyl-5-phenyl-pyrazolin-3-yl amide derivative 3 | Drug Info | [19] | |||
| 64 | Piperazine derivative 1 | Drug Info | [19] | |||
| 65 | Piperazine derivative 2 | Drug Info | [19] | |||
| 66 | PMID26161824-Compound-68 | Drug Info | [19] | |||
| 67 | PMID26161824-Compound-69 | Drug Info | [19] | |||
| 68 | Purine derivative 1 | Drug Info | [19] | |||
| 69 | Purine derivative 2 | Drug Info | [19] | |||
| 70 | Purine derivative 3 | Drug Info | [19] | |||
| 71 | Pyrano[2,3-b]pyridine derivative 1 | Drug Info | [19] | |||
| 72 | Pyrano[2,3-b]pyridine derivative 2 | Drug Info | [19] | |||
| 73 | Pyrazole derivative 1 | Drug Info | [19] | |||
| 74 | Pyrazole derivative 11 | Drug Info | [19] | |||
| 75 | Pyrazole derivative 12 | Drug Info | [19] | |||
| 76 | Pyrazole derivative 13 | Drug Info | [19] | |||
| 77 | Pyrazole derivative 14 | Drug Info | [19] | |||
| 78 | Pyrazole derivative 15 | Drug Info | [19] | |||
| 79 | Pyrazole derivative 16 | Drug Info | [19] | |||
| 80 | Pyrazole derivative 17 | Drug Info | [19] | |||
| 81 | Pyrazole derivative 18 | Drug Info | [19] | |||
| 82 | Pyrazole derivative 19 | Drug Info | [19] | |||
| 83 | Pyrazole derivative 2 | Drug Info | [19] | |||
| 84 | Pyrazole derivative 20 | Drug Info | [19] | |||
| 85 | Pyrazole derivative 21 | Drug Info | [19] | |||
| 86 | Pyrazole derivative 22 | Drug Info | [19] | |||
| 87 | Pyrazole derivative 23 | Drug Info | [19] | |||
| 88 | Pyrazole derivative 24 | Drug Info | [19] | |||
| 89 | Pyrazole derivative 25 | Drug Info | [19] | |||
| 90 | Pyrazole derivative 26 | Drug Info | [19] | |||
| 91 | Pyrazole derivative 27 | Drug Info | [19] | |||
| 92 | Pyrazole derivative 28 | Drug Info | [19] | |||
| 93 | Pyrazole derivative 29 | Drug Info | [19] | |||
| 94 | Pyrazole derivative 3 | Drug Info | [19] | |||
| 95 | Pyrazole derivative 30 | Drug Info | [19] | |||
| 96 | Pyrazole derivative 31 | Drug Info | [19] | |||
| 97 | Pyrazole derivative 32 | Drug Info | [19] | |||
| 98 | Pyrazole derivative 33 | Drug Info | [19] | |||
| 99 | Pyrazole derivative 34 | Drug Info | [19] | |||
| 100 | Pyrazole derivative 35 | Drug Info | [19] | |||
| 101 | Pyrazole derivative 36 | Drug Info | [19] | |||
| 102 | Pyrazole derivative 37 | Drug Info | [19] | |||
| 103 | Pyrazole derivative 38 | Drug Info | [19] | |||
| 104 | Pyrazole derivative 39 | Drug Info | [19] | |||
| 105 | Pyrazole derivative 4 | Drug Info | [19] | |||
| 106 | Pyrazole derivative 40 | Drug Info | [19] | |||
| 107 | Pyrazole derivative 5 | Drug Info | [19] | |||
| 108 | Pyrazole derivative 53 | Drug Info | [19] | |||
| 109 | Pyrazole derivative 54 | Drug Info | [19] | |||
| 110 | Pyrazole derivative 57 | Drug Info | [19] | |||
| 111 | Pyrazole derivative 58 | Drug Info | [19] | |||
| 112 | Pyrazole derivative 59 | Drug Info | [19] | |||
| 113 | Pyrazole derivative 6 | Drug Info | [19] | |||
| 114 | Pyrazole derivative 60 | Drug Info | [19] | |||
| 115 | Pyrazole derivative 7 | Drug Info | [19] | |||
| 116 | Pyrazole derivative 8 | Drug Info | [19] | |||
| 117 | Pyrazoline derivative 1 | Drug Info | [19] | |||
| 118 | Pyrazoline derivative 10 | Drug Info | [19] | |||
| 119 | Pyrazoline derivative 11 | Drug Info | [19] | |||
| 120 | Pyrazoline derivative 2 | Drug Info | [19] | |||
| 121 | Pyrazoline derivative 3 | Drug Info | [19] | |||
| 122 | Pyrazoline derivative 4 | Drug Info | [19] | |||
| 123 | Pyrazoline derivative 5 | Drug Info | [19] | |||
| 124 | Pyrazolo[1,5-a]pyrimidine derivative 1 | Drug Info | [19] | |||
| 125 | Pyrazolo[1,5-a]pyrimidine derivative 10 | Drug Info | [19] | |||
| 126 | Pyrazolo[1,5-a]pyrimidine derivative 11 | Drug Info | [19] | |||
| 127 | Pyrazolo[1,5-a]pyrimidine derivative 12 | Drug Info | [19] | |||
| 128 | Pyrazolo[1,5-a]pyrimidine derivative 13 | Drug Info | [19] | |||
| 129 | Pyrazolo[1,5-a]pyrimidine derivative 2 | Drug Info | [19] | |||
| 130 | Pyrazolo[1,5-a]pyrimidine derivative 3 | Drug Info | [19] | |||
| 131 | Pyrazolo[1,5-a]pyrimidine derivative 4 | Drug Info | [19] | |||
| 132 | Pyrazolo[1,5-a]pyrimidine derivative 5 | Drug Info | [19] | |||
| 133 | Pyrazolo[1,5-a]pyrimidine derivative 6 | Drug Info | [19] | |||
| 134 | Pyrazolo[1,5-a]pyrimidine derivative 7 | Drug Info | [19] | |||
| 135 | Pyrazolo[1,5-a]pyrimidine derivative 8 | Drug Info | [19] | |||
| 136 | Pyrazolo[1,5-a]pyrimidine derivative 9 | Drug Info | [19] | |||
| 137 | Pyridotriazolopyrimidine derivative 1 | Drug Info | [19] | |||
| 138 | Pyridotriazolopyrimidine derivative 2 | Drug Info | [19] | |||
| 139 | Pyridotriazolopyrimidine derivative 3 | Drug Info | [19] | |||
| 140 | Pyrido[2,3-d]pyrimidine derivative 1 | Drug Info | [19] | |||
| 141 | Pyrido[2,3-d]pyrimidine derivative 2 | Drug Info | [19] | |||
| 142 | Pyrrole derivative 1 | Drug Info | [19] | |||
| 143 | Pyrrole derivative 2 | Drug Info | [19] | |||
| 144 | Pyrrole derivative 3 | Drug Info | [19] | |||
| 145 | Pyrrole derivative 4 | Drug Info | [19] | |||
| 146 | Pyrrole derivative 5 | Drug Info | [19] | |||
| 147 | Pyrrole derivative 6 | Drug Info | [19] | |||
| 148 | Sulfonamide derivative 1 | Drug Info | [19] | |||
| 149 | Sulfonylated piperazine derivative 1 | Drug Info | [19] | |||
| 150 | Sulfonylated piperazine derivative 2 | Drug Info | [19] | |||
| 151 | Sulfonylated piperazine derivative 3 | Drug Info | [19] | |||
| 152 | Sulfonylated piperazine derivative 4 | Drug Info | [19] | |||
| 153 | Sulfonylated piperazine derivative 5 | Drug Info | [19] | |||
| 154 | Tetra-hydro-1H-1,2,6-triazaazulene derivative 1 | Drug Info | [19] | |||
| 155 | Tetra-hydro-1H-1,2,6-triazaazulene derivative 2 | Drug Info | [19] | |||
| 156 | CP-945598 | Drug Info | [47] | |||
| 157 | Taranabant | Drug Info | [35] | |||
| 158 | AVE1625 | Drug Info | [48] | |||
| 159 | AZD2207 | Drug Info | [42], [49] | |||
| 160 | SLV319 | Drug Info | [51] | |||
| 161 | AZD1175 | Drug Info | [42] | |||
| 162 | AZD1704 | Drug Info | [42] | |||
| 163 | CBD cannabis derivative | Drug Info | [30] | |||
| 164 | CB1 antagonist, Bayer | Drug Info | [21] | |||
| 165 | AM251 | Drug Info | [78] | |||
| 166 | BMS-812204 | Drug Info | [80] | |||
| 167 | CXB-029 | Drug Info | [80] | |||
| 168 | LY320135 | Drug Info | [90] | |||
| 169 | Methanandamide | Drug Info | [91] | |||
| 170 | PMID26161824C70 | Drug Info | [19] | |||
| 171 | [123I]AM251 | Drug Info | [104] | |||
| Modulator | [+] 5 Modulator drugs | + | ||||
| 1 | GW-42004 | Drug Info | [43] | |||
| 2 | SR-147778 | Drug Info | [45] | |||
| 3 | KN-38-7271 | Drug Info | [50] | |||
| 4 | PF-514273 | Drug Info | [52] | |||
| 5 | TAK-937 | Drug Info | [53] | |||
| Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
| 1 | Org27569 | Drug Info | [99] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: [3H]CP55940 | Ligand Info | |||||
| Structure Description | Cryo-EM structure of human receptor with G proteins | PDB:7WV9 | ||||
| Method | Electron microscopy | Resolution | 3.36 Å | Mutation | Yes | [108] |
| PDB Sequence |
ECFMVLNPSQ
115 QLAIAVLSLT125 LGTFTVLENL135 LVLCVILHSR145 SLRCRPSYHF155 IGSLAVADLL 165 GSVIFVYSFI175 DFHVFHRKDS185 RNVFLFKLGG195 VTASFTASVG205 SLFLTAIDRY 215 ISIHRPLAYK225 RIVTRPKAVV235 AFCLMWTIAI245 VIAVLPLLGW255 NCEKLQSVCS 265 DIFPHIDETY275 LMFWIGVTSV285 LLLFIVYAYM295 YILWKAHSHA305 VRMIQRGTQK 315 PDQARMDIRL341 AKTLVLILVV351 LIICWGPLLA361 IMVYDVFGKM371 NKLIKTVFAF 381 CSMLCLLNST391 VNPIIYALRS401 KDLRHAFRSM411
|
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|
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PHE170
3.517
SER173
2.561
PHE174
3.354
PHE177
3.540
HIS178
4.792
PHE189
4.757
LYS192
4.461
LEU193
3.586
VAL196
3.806
THR197
3.280
|
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| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Cannabinoid Receptor 1-G Protein Complex | PDB:6N4B | ||||
| Method | Electron microscopy | Resolution | 3.00 Å | Mutation | No | [109] |
| PDB Sequence |
MVLNPSQQLA
118 IAVLSLTLGT128 FTVLENLLVL138 CVILHSRSLR148 CRPSYHFIGS158 LAVADLLGSV 168 IFVYSFIDFH178 VFHRKDSRNV188 FLFKLGGVTA198 SFTASVGSLF208 LTAIDRYISI 218 HRPLAYKRIV228 TRPKAVVAFC238 LMWTIAIVIA248 VLPLLGWNCC264 SDIFPHIDET 274 YLMFWIGVTS284 VLLLFIVYAY294 MYILWKAHSH304 AVRMIQRGTA335 RMDIRLAKTL 345 VLILVVLIIC355 WGPLLAIMVY365 DVFGKMNKLI375 KTVFAFCSML385 CLLNSTVNPI 395 IYALRSKDLR405 HAFRSM
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
|
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Rap1 signaling pathway | hsa04015 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Thermogenesis | hsa04714 | Affiliated Target |
|
| Class: Organismal Systems => Environmental adaptation | Pathway Hierarchy | ||
| Retrograde endocannabinoid signaling | hsa04723 | Affiliated Target |
|
| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Degree | 7 | Degree centrality | 7.52E-04 | Betweenness centrality | 9.70E-04 |
|---|---|---|---|---|---|
| Closeness centrality | 2.04E-01 | Radiality | 1.36E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 1.01E+01 | Topological coefficient | 1.55E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Rap1 signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Retrograde endocannabinoid signaling | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Endogenous cannabinoid signaling | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | N-cadherin signaling events | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Class A/1 (Rhodopsin-like receptors) | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 6 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Small Ligand GPCRs | |||||
| 3 | BDNF signaling pathway | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| 6 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol. 2009 Feb;156(3):397-411. | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018651. | |||||
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| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5277). | |||||
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| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007737) | |||||
| REF 8 | ClinicalTrials.gov (NCT03788967) Study to Assess the Efficacy, Safety and Pharmacokinetics of Orally Administered Tebipenem Pivoxil Hydrobromide (SPR994) Compared to Intravenous Ertapenem in Patients With Complicated Urinary Tract Infection (cUTI) or Acute Pyelonephritis (AP) (ADAPT-PO). U.S. National Institutes of Health. | |||||
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| REF 12 | ClinicalTrials.gov (NCT03900325) Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Exploratory Efficacy of Nimacimab in Patients With Diabetic Gastroparesis. U.S. National Institutes of Health. | |||||
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| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025707) | |||||
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| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017654) | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024090) | |||||
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| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030875) | |||||
| REF 33 | 2011 Pipeline of Jenrin Discovery. | |||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143) | |||||
| REF 35 | Central side-effects of therapies based on CB1 cannabinoid receptor agonists and antagonists: focus on anxiety and depression. Best Pract Res Clin Endocrinol Metab. 2009 Feb;23(1):133-44. | |||||
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| REF 38 | Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50. | |||||
| REF 39 | The endogenous cannabinoid system protects against colonic inflammation. J Clin Invest. 2004 Apr;113(8):1202-9. | |||||
| REF 40 | Antinociceptive activity of the endogenous fatty acid amide, palmitylethanolamide. Eur J Pharmacol. 2001 May 11;419(2-3):191-8. | |||||
| REF 41 | Clinical pipeline report, company report or official report of Affimed Therapeutics. | |||||
| REF 42 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
| REF 43 | Company report (Gwpharm) | |||||
| REF 44 | Clinical pipeline report, company report or official report of Bird Rock Bio. | |||||
| REF 45 | Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits 9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans.Br J Clin Pharmacol.2013 Jul;76(1):65-77. | |||||
| REF 46 | Cannabinoid receptor antagonists: pharmacological opportunities, clinical experience, and translational prognosis. Expert Opin Emerg Drugs. 2009 Mar;14(1):43-65. | |||||
| REF 47 | Pfizer. Product Development Pipeline. March 31 2009. | |||||
| REF 48 | Pharma & Vaccines. Product Development Pipeline. April 29 2009. | |||||
| REF 49 | Ghrelin agonist TZP-101/ulimorelin accelerates gastrointestinal recovery independently of opioid use and surgery type: covariate analysis of phase 2 data. World J Surg. 2012 Jan;36(1):39-45. | |||||
| REF 50 | BAY 38-7271: a novel highly selective and highly potent cannabinoid receptor agonist for the treatment of traumatic brain injury.CNS Drug Rev.2003 Winter;9(4):343-58. | |||||
| REF 51 | JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6173-80. | |||||
| REF 52 | Effects of the novel cannabinoid CB1 receptor antagonist PF 514273 on the acquisition and expression of ethanol conditioned place preference. Alcohol. 2014 Aug;48(5):427-31. | |||||
| REF 53 | Cerebroprotective effects of TAK-937, a cannabinoid receptor agonist, on ischemic brain damage in middle cerebral artery occluded rats and non-human primates. Brain Res. 2012 Jan 9;1430:93-100. | |||||
| REF 54 | Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. | |||||
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| REF 56 | Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes. J Med Chem. 2009 May 14;52(9):3001-9. | |||||
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| REF 58 | Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach. Eur J Med Chem. 2010 Mar;45(3):1133-9. | |||||
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