Target Information
Target General Information | Top | |||||
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Target ID |
T47768
(Former ID: TTDS00126)
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Target Name |
Opioid receptor mu (MOP)
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Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Gene Name |
OPRM1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 13 Target-related Diseases | + | ||||
1 | Acute pain [ICD-11: MG31] | |||||
2 | Bowel habit change [ICD-11: ME05] | |||||
3 | Chronic pain [ICD-11: MG30] | |||||
4 | Corneal disease [ICD-11: 9A76-9A78] | |||||
5 | Cough [ICD-11: MD12] | |||||
6 | Depression [ICD-11: 6A70-6A7Z] | |||||
7 | Digestive system disease [ICD-11: DE2Z] | |||||
8 | Irritable bowel syndrome [ICD-11: DD91] | |||||
9 | Large intestine motility disorder [ICD-11: DB32] | |||||
10 | Opioid use disorder [ICD-11: 6C43] | |||||
11 | Pain [ICD-11: MG30-MG3Z] | |||||
12 | Pruritus [ICD-11: EC90] | |||||
13 | Sensation disturbance [ICD-11: MB40] | |||||
Function |
Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B. Also couples to adenylate cyclase stimulatory G alpha proteins. The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4. Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization. Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction. The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins. The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation. Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling. Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling. Endogenous ligands induce rapid desensitization, endocytosis and recycling whereas morphine induces only low desensitization and endocytosis. Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties. Involved in neurogenesis. Isoform 12 couples to GNAS and is proposed to be involved in excitatory effects. Isoform 16 and isoform 17 do not bind agonists but may act through oligomerization with binding-competent OPRM1 isoforms and reduce their ligand binding activity. Receptor for endogenous opioids such as beta-endorphin and endomorphin.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00768 ; BADD_A01328 ; BADD_A03957 ; BADD_A05200 ; BADD_A06356 | |||||
HIT2.0 ID | T66YJ0 |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 24 Approved Drugs | + | ||||
1 | Alfentanil | Drug Info | Approved | Anaesthesia | [2], [3] | |
2 | Alvimopan | Drug Info | Approved | Gastrointestinal disease | [4], [5], [6] | |
3 | Anileridine | Drug Info | Approved | Pain | [7], [8] | |
4 | Anileridine Hydrochloride | Drug Info | Approved | Pain | [9] | |
5 | Buprenorphine | Drug Info | Approved | Pain | [10], [11] | |
6 | Buprenorphine + naloxone | Drug Info | Approved | Opioid dependence | [9] | |
7 | Diphenoxylate | Drug Info | Approved | Diarrhea | [12], [13] | |
8 | Eluxadoline | Drug Info | Approved | Diarrhea-predominant irritable bowel syndrome | [14], [15] | |
9 | Fentanyl | Drug Info | Approved | Analgesia | [9] | |
10 | Hydrocodone | Drug Info | Approved | Pain | [16], [17] | |
11 | Hydromorphone | Drug Info | Approved | Pain | [9] | |
12 | Levomethadyl Acetate | Drug Info | Approved | Opioid dependence | [18], [19] | |
13 | Levopropoxyphene Napsylate Anhydrous | Drug Info | Approved | Cough | [9] | |
14 | Methadyl Acetate | Drug Info | Approved | Opioid dependence | [20] | |
15 | Methylnaltrexone bromide | Drug Info | Approved | Opioid-induced constipation | [5] | |
16 | Morphine | Drug Info | Approved | Chronic pain | [9] | |
17 | Naldemedine Tosylate | Drug Info | Approved | Opioid-induced constipation | [21], [22] | |
18 | Nalfurafine hcl | Drug Info | Approved | Uremic pruritus | [9] | |
19 | Naloxegol | Drug Info | Approved | Opioid-induced constipation | [9], [23], [24] | |
20 | Naloxone | Drug Info | Approved | Narcotic depression | [25], [26] | |
21 | Oxycodone | Drug Info | Approved | Pain | [27], [28] | |
22 | Propoxyphene Hydrochloride | Drug Info | Approved | Pain | [9] | |
23 | Remifentanil | Drug Info | Approved | Anaesthesia | [29], [30] | |
24 | Tapentadol hydrochloride | Drug Info | Approved | Acute pain | [5] | |
Clinical Trial Drug(s) | [+] 15 Clinical Trial Drugs | + | ||||
1 | GRT-6005 | Drug Info | Phase 3 | Diabetic neuropathy | [31] | |
2 | Morphine-6-glucuronide | Drug Info | Phase 3 | Pain | [32] | |
3 | NKTR-181 | Drug Info | Phase 3 | Neuropathic pain | [33] | |
4 | ALKS33 | Drug Info | Phase 2 | Alcohol dependence | [34] | |
5 | Met-enkephalin | Drug Info | Phase 2 | Pain | [35], [36] | |
6 | OPNT001 | Drug Info | Phase 2 | Eating disorder | [37] | |
7 | TD-1211 | Drug Info | Phase 2 | Opioid-induced constipation | [38] | |
8 | TPM-1/Morphine | Drug Info | Phase 2 | Pain | [39] | |
9 | AIKO-150 | Drug Info | Phase 1 | Opioid dependence | [40] | |
10 | Cyt-1010 | Drug Info | Phase 1 | Pain | [41] | |
11 | GSK1521498 | Drug Info | Phase 1 | Obesity | [42] | |
12 | MCP-201 | Drug Info | Phase 1 | Pain | [43] | |
13 | NOCICEPTIN | Drug Info | Phase 1 | Headache | [44] | |
14 | SALVINORIN A | Drug Info | Phase 1 | Cerebral vasospasm | [45], [33] | |
15 | TRV734 | Drug Info | Phase 1 | Chronic pain | [33] | |
Discontinued Drug(s) | [+] 15 Discontinued Drugs | + | ||||
1 | ADL-5945 | Drug Info | Discontinued in Phase 2 | Constipation | [46] | |
2 | BCH-2687 | Drug Info | Discontinued in Phase 2 | Pain | [47] | |
3 | DPI-3290 | Drug Info | Discontinued in Phase 2 | Pain | [48] | |
4 | Frakefamide | Drug Info | Discontinued in Phase 2 | Pain | [47] | |
5 | MIRFENTANIL HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Pain | [49] | |
6 | Transdur-sufentanil | Drug Info | Discontinued in Phase 2 | Pain | [50] | |
7 | TREFENTANIL HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Pain | [51] | |
8 | ADL-7445 | Drug Info | Discontinued in Phase 1 | Constipation | [52] | |
9 | KN-203 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [53] | |
10 | VP004 | Drug Info | Discontinued in Phase 1 | Substance use disorder | [54] | |
11 | 443C81 | Drug Info | Terminated | Asthma | [56] | |
12 | BCH-150 | Drug Info | Terminated | Gastrointestinal disease | [57] | |
13 | DBO-11 | Drug Info | Terminated | Cancer related pain | [58] | |
14 | DBO-17 | Drug Info | Terminated | Cancer related pain | [59] | |
15 | Sameridine | Drug Info | Terminated | Pain | [60] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | GNTI | Drug Info | Preclinical | Obesity | [55] | |
2 | LY-25582 | Drug Info | Preclinical | Obesity | [55] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Agonist | [+] 38 Agonist drugs | + | ||||
1 | Alfentanil | Drug Info | [61] | |||
2 | Anileridine | Drug Info | [63] | |||
3 | Buprenorphine | Drug Info | [65], [66] | |||
4 | Buprenorphine + naloxone | Drug Info | [67] | |||
5 | Diphenoxylate | Drug Info | [68] | |||
6 | Levomethadyl Acetate | Drug Info | [75] | |||
7 | Methadyl Acetate | Drug Info | [76] | |||
8 | Remifentanil | Drug Info | [1] | |||
9 | Morphine-6-glucuronide | Drug Info | [83] | |||
10 | NKTR-181 | Drug Info | [84] | |||
11 | Carfentanil | Drug Info | [86] | |||
12 | Cyt-1010 | Drug Info | [91] | |||
13 | GSK1521498 | Drug Info | [42], [92] | |||
14 | MCP-201 | Drug Info | [93] | |||
15 | TRV734 | Drug Info | [33] | |||
16 | BCH-2687 | Drug Info | [97] | |||
17 | DPI-3290 | Drug Info | [98] | |||
18 | Frakefamide | Drug Info | [100] | |||
19 | MIRFENTANIL HYDROCHLORIDE | Drug Info | [9], [101] | |||
20 | Transdur-sufentanil | Drug Info | [102] | |||
21 | TREFENTANIL HYDROCHLORIDE | Drug Info | [9], [103] | |||
22 | KN-203 | Drug Info | [104] | |||
23 | DBO-11 | Drug Info | [83] | |||
24 | DBO-17 | Drug Info | [83] | |||
25 | 3-Methylfentanyl | Drug Info | [128] | |||
26 | 3-Methylthiofentanyl | Drug Info | [129] | |||
27 | Dihydromorphine | Drug Info | [161] | |||
28 | Dimethylthiambutene | Drug Info | [162] | |||
29 | DSLET | Drug Info | [81] | |||
30 | dynorphin B | Drug Info | [81] | |||
31 | ethylketocyclazocine | Drug Info | [81] | |||
32 | Ethylmorphine | Drug Info | [171] | |||
33 | Etorphine | Drug Info | [173] | |||
34 | NE-2 | Drug Info | [81] | |||
35 | normorphine | Drug Info | [81] | |||
36 | NRP290 | Drug Info | [81] | |||
37 | PL017 | Drug Info | [152] | |||
38 | TQ-1017 | Drug Info | [9] | |||
Antagonist | [+] 21 Antagonist drugs | + | ||||
1 | Alvimopan | Drug Info | [62] | |||
2 | Naldemedine Tosylate | Drug Info | [22] | |||
3 | Naloxone | Drug Info | [79], [80] | |||
4 | OPNT001 | Drug Info | [37] | |||
5 | AIKO-150 | Drug Info | [74], [90] | |||
6 | ADL-5945 | Drug Info | [96] | |||
7 | ADL-7445 | Drug Info | [96] | |||
8 | GNTI | Drug Info | [55] | |||
9 | LY-25582 | Drug Info | [55], [106] | |||
10 | ADC-5510 | Drug Info | [81] | |||
11 | AIKO-151 | Drug Info | [81] | |||
12 | Beta-endorphin | Drug Info | [144] | |||
13 | CTAP | Drug Info | [152] | |||
14 | CTOP | Drug Info | [142], [153] | |||
15 | Diprenorphine | Drug Info | [163] | |||
16 | KIN-4044 | Drug Info | [81] | |||
17 | KRP-100 | Drug Info | [81] | |||
18 | naloxonazine | Drug Info | [153] | |||
19 | naltriben | Drug Info | [81] | |||
20 | quadazocine | Drug Info | [81] | |||
21 | [3H]diprenorphine | Drug Info | [153] | |||
Modulator | [+] 24 Modulator drugs | + | ||||
1 | Anileridine Hydrochloride | Drug Info | [64] | |||
2 | Eluxadoline | Drug Info | [69] | |||
3 | Fentanyl | Drug Info | [70], [71] | |||
4 | Hydrocodone | Drug Info | [72], [73] | |||
5 | Levopropoxyphene Napsylate Anhydrous | Drug Info | [64] | |||
6 | Methylnaltrexone bromide | Drug Info | [5] | |||
7 | Morphine | Drug Info | [77] | |||
8 | Naloxegol | Drug Info | [9], [24] | |||
9 | Oxycodone | Drug Info | [81] | |||
10 | Propoxyphene Hydrochloride | Drug Info | [82] | |||
11 | Tapentadol hydrochloride | Drug Info | [5] | |||
12 | GRT-6005 | Drug Info | [31] | |||
13 | TD-1211 | Drug Info | [88] | |||
14 | 443C81 | Drug Info | [107] | |||
15 | BCH-150 | Drug Info | [108] | |||
16 | Sameridine | Drug Info | [110] | |||
17 | AIKO-152 | Drug Info | [81] | |||
18 | Endomorphins | Drug Info | [81] | |||
19 | KIN-3031 | Drug Info | [81] | |||
20 | KRP-110 | Drug Info | [81] | |||
21 | NCT-400 | Drug Info | [81] | |||
22 | NRT-300 | Drug Info | [81] | |||
23 | PTI-601 | Drug Info | [81] | |||
24 | Semorphone | Drug Info | [210] | |||
Inhibitor | [+] 426 Inhibitor drugs | + | ||||
1 | Hydromorphone | Drug Info | [74] | |||
2 | Nalfurafine hcl | Drug Info | [78] | |||
3 | ALKS33 | Drug Info | [85] | |||
4 | Met-enkephalin | Drug Info | [87] | |||
5 | TPM-1/Morphine | Drug Info | [89] | |||
6 | NOCICEPTIN | Drug Info | [94] | |||
7 | SALVINORIN A | Drug Info | [95] | |||
8 | Dynorphin a | Drug Info | [99] | |||
9 | BIPHALIN | Drug Info | [109] | |||
10 | SB-213698 | Drug Info | [111] | |||
11 | SNF-9007 | Drug Info | [112] | |||
12 | (+/-)-nantenine | Drug Info | [113] | |||
13 | (+/-)-TRANS-U-50488 METHANESULFONATE | Drug Info | [114] | |||
14 | (-)-cyclorphan | Drug Info | [115] | |||
15 | (-)-eseroline | Drug Info | [114] | |||
16 | (H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) | Drug Info | [116] | |||
17 | 1,10-bis-(Dmt-Tic-amino)decane | Drug Info | [117] | |||
18 | 1,4-bis-(Dmt-Tic-amino)butane | Drug Info | [117] | |||
19 | 1,6-bis-(Dmt-Tic-amino)hexane | Drug Info | [117] | |||
20 | 1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane | Drug Info | [117] | |||
21 | 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [118] | |||
22 | 1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [118] | |||
23 | 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol | Drug Info | [118] | |||
24 | 1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol | Drug Info | [119] | |||
25 | 1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol | Drug Info | [119] | |||
26 | 1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol | Drug Info | [119] | |||
27 | 1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol | Drug Info | [119] | |||
28 | 1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol | Drug Info | [119] | |||
29 | 1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol | Drug Info | [119] | |||
30 | 1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol | Drug Info | [119] | |||
31 | 1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol | Drug Info | [119] | |||
32 | 1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol | Drug Info | [119] | |||
33 | 1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol | Drug Info | [119] | |||
34 | 1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol | Drug Info | [119] | |||
35 | 1-benzhydryl-4-(furan-2-yl)piperidin-4-ol | Drug Info | [119] | |||
36 | 1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol | Drug Info | [119] | |||
37 | 1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol | Drug Info | [119] | |||
38 | 1-benzhydryl-4-benzylpiperidin-4-ol | Drug Info | [119] | |||
39 | 1-benzhydryl-4-butylpiperidin-4-ol | Drug Info | [119] | |||
40 | 1-benzhydryl-4-cyclohexylpiperidin-4-ol | Drug Info | [119] | |||
41 | 1-benzhydryl-4-cyclopropylpiperidin-4-ol | Drug Info | [119] | |||
42 | 1-benzhydryl-4-ethoxy-4-phenylpiperidine | Drug Info | [118] | |||
43 | 1-benzhydryl-4-hexylpiperidin-4-ol | Drug Info | [119] | |||
44 | 1-benzhydryl-4-isopropylpiperidin-4-ol | Drug Info | [119] | |||
45 | 1-benzhydryl-4-m-tolylpiperidin-4-ol | Drug Info | [119] | |||
46 | 1-benzhydryl-4-methoxy-4-phenylpiperidine | Drug Info | [118] | |||
47 | 1-benzhydryl-4-o-tolylpiperidin-4-ol | Drug Info | [119] | |||
48 | 1-benzhydryl-4-p-tolylpiperidin-4-ol | Drug Info | [119] | |||
49 | 1-benzhydryl-4-phenyl-4-propoxypiperidine | Drug Info | [118] | |||
50 | 1-benzhydryl-4-phenylpiperidin-4-ol | Drug Info | [120] | |||
51 | 1-benzhydryl-4-tert-butylpiperidin-4-ol | Drug Info | [119] | |||
52 | 1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [121] | |||
53 | 1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [121] | |||
54 | 14-O-phenylpropylnaltrexone | Drug Info | [122] | |||
55 | 17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [123] | |||
56 | 17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [123] | |||
57 | 17-methyl-4'-methyldihydromorphinone | Drug Info | [124] | |||
58 | 17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate | Drug Info | [123] | |||
59 | 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide | Drug Info | [125] | |||
60 | 2-Benzylaminomethyl-3-hydroxymorphinan | Drug Info | [123] | |||
61 | 2-Hydroxymethyl-3-hydroxymorphinan | Drug Info | [123] | |||
62 | 3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone | Drug Info | [117] | |||
63 | 3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone | Drug Info | [117] | |||
64 | 3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone | Drug Info | [117] | |||
65 | 3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | Drug Info | [117] | |||
66 | 3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole | Drug Info | [126] | |||
67 | 3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol | Drug Info | [127] | |||
68 | 3-desoxy-3-carboxamidonaltrexone | Drug Info | [85] | |||
69 | 4-(4-((phenethylamino)methyl)phenoxy)benzamide | Drug Info | [130] | |||
70 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [131] | |||
71 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide | Drug Info | [132] | |||
72 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol | Drug Info | [133] | |||
73 | 4-phenyl-1-(1-phenylbutyl)piperidin-4-ol | Drug Info | [118] | |||
74 | 4-phenyl-1-(1-phenylethyl)piperidin-4-ol | Drug Info | [118] | |||
75 | 4-phenyl-1-(1-phenylheptyl)piperidin-4-ol | Drug Info | [118] | |||
76 | 4-phenyl-1-(1-phenylhexyl)piperidin-4-ol | Drug Info | [118] | |||
77 | 4-phenyl-1-(1-phenylpentyl)piperidin-4-ol | Drug Info | [118] | |||
78 | 4-phenyl-1-(1-phenylpropyl)piperidin-4-ol | Drug Info | [118] | |||
79 | 4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol | Drug Info | [118] | |||
80 | 4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol | Drug Info | [118] | |||
81 | 4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol | Drug Info | [118] | |||
82 | 5-(4-((phenethylamino)methyl)phenoxy)picolinamide | Drug Info | [130] | |||
83 | 6-(2-benzylisoindolin-5-yloxy)nicotinamide | Drug Info | [106] | |||
84 | 6-(2-phenethylisoindolin-5-yloxy)nicotinamide | Drug Info | [106] | |||
85 | 6-(4-((benzylamino)methyl)phenoxy)nicotinamide | Drug Info | [130] | |||
86 | 6-(4-((phenethylamino)methyl)phenoxy)nicotinamide | Drug Info | [106] | |||
87 | 6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide | Drug Info | [106] | |||
88 | 6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide | Drug Info | [130] | |||
89 | 6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide | Drug Info | [130] | |||
90 | 6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol | Drug Info | [134] | |||
91 | 6-desoxonaltrexone | Drug Info | [85] | |||
92 | 6beta-naltrexol HCl | Drug Info | [135] | |||
93 | 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide | Drug Info | [136] | |||
94 | 8-carboxamidocyclazocine | Drug Info | [137] | |||
95 | Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 | Drug Info | [138] | |||
96 | Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 | Drug Info | [138] | |||
97 | Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG | Drug Info | [139] | |||
98 | Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG | Drug Info | [139] | |||
99 | Ac-RYYRIK-K-(NH2)-YAFGYPS | Drug Info | [139] | |||
100 | Ac-RYYRIK-K-(NH2)-YRFB | Drug Info | [139] | |||
101 | Ac-YGGFL-NH2 | Drug Info | [140] | |||
102 | AKUAMMINE | Drug Info | [114] | |||
103 | AMINOFENTANYL | Drug Info | [141] | |||
104 | Antanal 1 | Drug Info | [142] | |||
105 | Antanal 2 | Drug Info | [142] | |||
106 | Benzyl derivative of M6G | Drug Info | [143] | |||
107 | Beta-funaltrexamine | Drug Info | [145] | |||
108 | Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate | Drug Info | [115] | |||
109 | BREMAZOCINE | Drug Info | [146] | |||
110 | BUTORPHAN | Drug Info | [147] | |||
111 | C6S | Drug Info | [148] | |||
112 | CARBOXYFENTANYL | Drug Info | [149] | |||
113 | Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [150] | |||
114 | Clocinnamox | Drug Info | [122] | |||
115 | CODEINONE | Drug Info | [151] | |||
116 | CYCLAZOCINE | Drug Info | [147] | |||
117 | CYCLORPHAN | Drug Info | [147] | |||
118 | CYPRODIME | Drug Info | [154] | |||
119 | C[L-Ala-D-pro-L-Phe-D-trp] | Drug Info | [138] | |||
120 | C[L-mTyr-D-pro-L-Phe-D-trp] | Drug Info | [138] | |||
121 | C[L-Phe-D-pro-L-mTyr-D-trp] | Drug Info | [138] | |||
122 | C[L-Phe-D-pro-L-Phe-D-trp] | Drug Info | [138] | |||
123 | C[L-Phe-D-pro-L-Phe-L-trp] | Drug Info | [138] | |||
124 | C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] | Drug Info | [138] | |||
125 | C[L-Phe-D-pro-L-Tyr-D-trp] | Drug Info | [138] | |||
126 | C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] | Drug Info | [138] | |||
127 | C[L-Tyr-D-pro-L-Phe-D-trp] | Drug Info | [138] | |||
128 | D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | [155] | |||
129 | D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) | Drug Info | [155] | |||
130 | D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) | Drug Info | [155] | |||
131 | D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | [155] | |||
132 | DADLE | Drug Info | [156] | |||
133 | DAMGO | Drug Info | [157] | |||
134 | DC6S | Drug Info | [148] | |||
135 | Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [158] | |||
136 | DELTORPHIN | Drug Info | [159] | |||
137 | DELTORPHIN-II | Drug Info | [160] | |||
138 | Deprotected cogener of M6G | Drug Info | [143] | |||
139 | DERMORPHIN | Drug Info | [139] | |||
140 | Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [158] | |||
141 | DIHYDROAKUAMMINE | Drug Info | [114] | |||
142 | Dimepheptanol | Drug Info | [134] | |||
143 | DM3A6S | Drug Info | [148] | |||
144 | DM3B6S | Drug Info | [148] | |||
145 | DM6S | Drug Info | [148] | |||
146 | Dmt-Pro-3,5Dmp-Phe-NH2 | Drug Info | [164] | |||
147 | Dmt-Pro-Dmp-Phe-NH2 | Drug Info | [164] | |||
148 | Dmt-Pro-Dmt-Phe-NH2 | Drug Info | [164] | |||
149 | Dmt-Pro-Emp-Phe-NH2 | Drug Info | [164] | |||
150 | Dmt-Pro-Imp-Phe-NH2 | Drug Info | [164] | |||
151 | Dmt-Pro-Mmp-Phe-NH2 | Drug Info | [164] | |||
152 | Dmt-Pro-Phe-D-1-Nal-NH2 | Drug Info | [165] | |||
153 | Dmt-Pro-Phe-D-2-Nal-NH2 | Drug Info | [165] | |||
154 | Dmt-Pro-Phe-Phe-NH2 | Drug Info | [164] | |||
155 | Dmt-Pro-Tmp-Phe-NH2 | Drug Info | [164] | |||
156 | Dmt-Pro-Trp-D-2-Nal-NH2 | Drug Info | [165] | |||
157 | Dmt-Sar-Phe-D-2-Nal-NH | Drug Info | [166] | |||
158 | DPDPE | Drug Info | [157] | |||
159 | Dynorphin(1-8) | Drug Info | [167] | |||
160 | ELAEOCARPENINE | Drug Info | [168] | |||
161 | ENDOMORPHIN 2 | Drug Info | [169] | |||
162 | ENDOMORPHIN-1 | Drug Info | [170] | |||
163 | ETONITAZENE | Drug Info | [172] | |||
164 | FALCARINDIOL | Drug Info | [174] | |||
165 | FLUPERAMIDE | Drug Info | [175] | |||
166 | H-2',6'-dimethyltyrosine-Tic-OH | Drug Info | [176] | |||
167 | H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH | Drug Info | [176] | |||
168 | H-Aba-ala-Gly-Phe-leu-OH | Drug Info | [87] | |||
169 | H-Aba-ala-Gly-Phe-Met-OH | Drug Info | [87] | |||
170 | H-Aba-Gly-Gly-Phe-Leu-OH | Drug Info | [87] | |||
171 | H-Aba-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [87] | |||
172 | H-Apa-ala-Gly-Phe-leu-OH | Drug Info | [87] | |||
173 | H-Cdp-ala-Gly-Phe-leu-OH | Drug Info | [87] | |||
174 | H-Cdp-Gly-Gly-Phe-Leu-OH | Drug Info | [87] | |||
175 | H-Cdp-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [87] | |||
176 | H-Cpa-Gly-Gly-Phe-Met-NH2 | Drug Info | [87] | |||
177 | H-Cpa-Gly-Gly-Phe-Met-OH | Drug Info | [87] | |||
178 | H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [177] | |||
179 | H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [177] | |||
180 | H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [177] | |||
181 | H-Dmt-Aba-Gly-NH-CH2-Bid | Drug Info | [178] | |||
182 | H-Dmt-Aba-Gly-NH-CH2-Ph | Drug Info | [178] | |||
183 | H-Dmt-Aba-Gly-NH-Ph | Drug Info | [178] | |||
184 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 | Drug Info | [179] | |||
185 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH | Drug Info | [179] | |||
186 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 | Drug Info | [180] | |||
187 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH | Drug Info | [180] | |||
188 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 | Drug Info | [180] | |||
189 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH | Drug Info | [180] | |||
190 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 | Drug Info | [180] | |||
191 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH | Drug Info | [180] | |||
192 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 | Drug Info | [180] | |||
193 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH | Drug Info | [180] | |||
194 | H-Dmt-Tic-Asp-N(Me)-Ph | Drug Info | [181] | |||
195 | H-Dmt-Tic-Asp-NH-Bzl | Drug Info | [181] | |||
196 | H-Dmt-Tic-Asp-NH-Ph | Drug Info | [181] | |||
197 | H-Dmt-Tic-D-Asp-N(Me)-Ph | Drug Info | [181] | |||
198 | H-Dmt-Tic-D-Asp-NH-Ph | Drug Info | [181] | |||
199 | H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) | Drug Info | [116] | |||
200 | H-Dmt-Tic-Glu-NH-(CH2)5-NH2 | Drug Info | [182] | |||
201 | H-Dmt-Tic-Glu-NH2 | Drug Info | [182] | |||
202 | H-Dmt-Tic-Gly-N(Me)-Ph | Drug Info | [181] | |||
203 | H-Dmt-Tic-Gly-NH-Bzl | Drug Info | [181] | |||
204 | H-Dmt-Tic-Gly-NH-CH2-Bid | Drug Info | [178] | |||
205 | H-Dmt-Tic-Gly-NH-Ph | Drug Info | [181] | |||
206 | H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph | Drug Info | [183] | |||
207 | H-Dmt-Tic-Lys(Ac)-NH-Ph | Drug Info | [183] | |||
208 | H-Dmt-Tic-Lys(Z)-NH-CH2-Ph | Drug Info | [183] | |||
209 | H-Dmt-Tic-Lys(Z)-NH-Ph | Drug Info | [183] | |||
210 | H-Dmt-Tic-Lys-NH-CH2-Ph | Drug Info | [183] | |||
211 | H-Dmt-Tic-Lys-NH-Ph | Drug Info | [183] | |||
212 | H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H | Drug Info | [184] | |||
213 | H-Dmt-Tic-NH-(CH2)6-NH-Phe-H | Drug Info | [184] | |||
214 | H-Dmt-Tic-NH-(CH2)6-NH-Tic-H | Drug Info | [184] | |||
215 | H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid | Drug Info | [183] | |||
216 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid | Drug Info | [181] | |||
217 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [181] | |||
218 | H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [181] | |||
219 | H-Dmt-Tic-NH-CH2-Boa | Drug Info | [185] | |||
220 | H-Dmt-Tic-NH-CH2-Bta | Drug Info | [185] | |||
221 | H-Dmt-Tic-NH-CH2-CH2-NH2 | Drug Info | [186] | |||
222 | H-Dmt-Tic-NH-CH2-Imid | Drug Info | [185] | |||
223 | H-Dmt-Tic-NH-CH2-ImidPh | Drug Info | [185] | |||
224 | H-Dmt-Tic-NH-CH2-Indl | Drug Info | [185] | |||
225 | H-Dmt-Tic-NH-CH2-Indn | Drug Info | [185] | |||
226 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid | Drug Info | [183] | |||
227 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid | Drug Info | [183] | |||
228 | H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid | Drug Info | [183] | |||
229 | H-mCpa-ala-Gly-Phe-leu-OH | Drug Info | [87] | |||
230 | H-mCpa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [87] | |||
231 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH | Drug Info | [150] | |||
232 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 | Drug Info | [187] | |||
233 | H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 | Drug Info | [187] | |||
234 | H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 | Drug Info | [187] | |||
235 | H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 | Drug Info | [187] | |||
236 | H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 | Drug Info | [188] | |||
237 | H-Tyr-c[D-Orn-Aic-Glu]-NH2 | Drug Info | [188] | |||
238 | H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 | Drug Info | [189] | |||
239 | H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 | Drug Info | [189] | |||
240 | H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Drug Info | [190] | |||
241 | H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac | Drug Info | [191] | |||
242 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H | Drug Info | [192] | |||
243 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [192] | |||
244 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [192] | |||
245 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc | Drug Info | [191] | |||
246 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [191] | |||
247 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [191] | |||
248 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [191] | |||
249 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | [192] | |||
250 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Drug Info | [190] | |||
251 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Drug Info | [190] | |||
252 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Drug Info | [190] | |||
253 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Drug Info | [190] | |||
254 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Drug Info | [190] | |||
255 | H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 | Drug Info | [189] | |||
256 | H-Tyr-Gly-Gly-Phe-Met-NH2 | Drug Info | [87] | |||
257 | H-Tyr-Pro-Ala-Phe-NH2 | Drug Info | [140] | |||
258 | H-Tyr-Pro-Dap(6DMN)-Phe-NH2 | Drug Info | [116] | |||
259 | H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 | Drug Info | [116] | |||
260 | H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H | Drug Info | [186] | |||
261 | H-Tyr-Tic-Cha-Phe-OH | Drug Info | [180] | |||
262 | H-Tyr-Tic-Phe-Phe-OH | Drug Info | [180] | |||
263 | HERKINORIN | Drug Info | [95] | |||
264 | HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 | Drug Info | [193] | |||
265 | ICI-199441 | Drug Info | [194] | |||
266 | KETOCYCLAZOCINE | Drug Info | [90] | |||
267 | KNT-5 | Drug Info | [195] | |||
268 | KNT-62 | Drug Info | [78] | |||
269 | KNT-63 | Drug Info | [78] | |||
270 | Leucine-enkephalin | Drug Info | [167] | |||
271 | LOFENTANIL | Drug Info | [196] | |||
272 | M3A6S | Drug Info | [148] | |||
273 | M3B6S | Drug Info | [148] | |||
274 | M3IBu6S | Drug Info | [148] | |||
275 | M3P6S | Drug Info | [148] | |||
276 | M3Pr6S | Drug Info | [148] | |||
277 | M3S | Drug Info | [148] | |||
278 | M6G thiosaccharide analogue | Drug Info | [143] | |||
279 | M6S | Drug Info | [148] | |||
280 | MC-CAM | Drug Info | [197] | |||
281 | MCL-117 | Drug Info | [115] | |||
282 | MCL-139 | Drug Info | [115] | |||
283 | MCL-144 | Drug Info | [198] | |||
284 | MCL-145 | Drug Info | [115] | |||
285 | MCL-147 | Drug Info | [199] | |||
286 | MCL-149 | Drug Info | [199] | |||
287 | MCL-153 | Drug Info | [200] | |||
288 | MCL-154 | Drug Info | [200] | |||
289 | MCL-182 | Drug Info | [199] | |||
290 | MCL-183 | Drug Info | [199] | |||
291 | MCL-428 | Drug Info | [201] | |||
292 | MCL-429 | Drug Info | [201] | |||
293 | MCL-431 | Drug Info | [201] | |||
294 | MCL-432 | Drug Info | [201] | |||
295 | MCL-433 | Drug Info | [201] | |||
296 | MCL-434 | Drug Info | [201] | |||
297 | MCL-435 | Drug Info | [201] | |||
298 | MCL-443 | Drug Info | [201] | |||
299 | MCL-444 | Drug Info | [201] | |||
300 | MCL-445 | Drug Info | [199] | |||
301 | MCL-446 | Drug Info | [199] | |||
302 | MCL-447 | Drug Info | [199] | |||
303 | MCL-448 | Drug Info | [199] | |||
304 | MCL-449 | Drug Info | [201] | |||
305 | MCL-450 | Drug Info | [202] | |||
306 | MCL-451 | Drug Info | [202] | |||
307 | MCL-457 | Drug Info | [199] | |||
308 | MCL-458 | Drug Info | [199] | |||
309 | METAZOCINE | Drug Info | [203] | |||
310 | MM3A6S | Drug Info | [148] | |||
311 | MM3B6S | Drug Info | [148] | |||
312 | MORPHICEPTIN | Drug Info | [169] | |||
313 | MORPHINONE | Drug Info | [151] | |||
314 | MR-1029 | Drug Info | [204] | |||
315 | MR-1526 | Drug Info | [204] | |||
316 | MR-2034 | Drug Info | [90] | |||
317 | MR-2266 | Drug Info | [204] | |||
318 | N-(17-Methylmorphinan-3-yl)-N'-phenylurea | Drug Info | [123] | |||
319 | N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea | Drug Info | [123] | |||
320 | N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 | Drug Info | [205] | |||
321 | N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 | Drug Info | [205] | |||
322 | N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 | Drug Info | [205] | |||
323 | N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine | Drug Info | [123] | |||
324 | N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine | Drug Info | [123] | |||
325 | N-isobutylnoroxymorphone | Drug Info | [206] | |||
326 | NalBzOH | Drug Info | [148] | |||
327 | Naltrexone-6-alpha-ol | Drug Info | [90] | |||
328 | NORBINALTORPHIMINE | Drug Info | [207] | |||
329 | O-DESMETHYL TRAMADOL | Drug Info | [90] | |||
330 | ORIPAVINE | Drug Info | [151] | |||
331 | OXYMORPHINDOLE | Drug Info | [172] | |||
332 | Oxymorphone semicarbazone hydrochloride | Drug Info | [167] | |||
333 | PHENAZOCINE | Drug Info | [90] | |||
334 | RTI-5989-31 | Drug Info | [208] | |||
335 | SB-0304 | Drug Info | [209] | |||
336 | SL-3111 | Drug Info | [211] | |||
337 | SN-11 | Drug Info | [111] | |||
338 | SN-23 | Drug Info | [111] | |||
339 | SN-28 | Drug Info | [212] | |||
340 | SOMATOSTATIN | Drug Info | [155] | |||
341 | SPIROINDANYLOXYMORPHONE | Drug Info | [213] | |||
342 | THEBAINE | Drug Info | [151] | |||
343 | Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [150] | |||
344 | Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 | Drug Info | [214] | |||
345 | Tyr-(R)-Aba-Gly-Phe-NH2 | Drug Info | [215] | |||
346 | Tyr-(R)-spiro-Aba-Gly-Phe-NH2 | Drug Info | [215] | |||
347 | Tyr-(S)-Aba-Gly-Phe-NH2 | Drug Info | [215] | |||
348 | Tyr-(S)-spiro-Aba-Gly-Phe-NH2 | Drug Info | [215] | |||
349 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
350 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
351 | Tyr-D-Ala-Gly-NMePhe | Drug Info | [145] | |||
352 | Tyr-D-Ala-Gly-Phe-Met-NH2 | Drug Info | [109] | |||
353 | Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Drug Info | [216] | |||
354 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [191] | |||
355 | Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
356 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
357 | Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 | Drug Info | [217] | |||
358 | Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 | Drug Info | [218] | |||
359 | Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 | Drug Info | [217] | |||
360 | Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 | Drug Info | [217] | |||
361 | Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 | Drug Info | [217] | |||
362 | Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 | Drug Info | [218] | |||
363 | Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
364 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
365 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
366 | Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
367 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
368 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
369 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [112] | |||
370 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
371 | Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
372 | Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [112] | |||
373 | Tyr-Pro-3,5Dmp-Phe-NH2 | Drug Info | [164] | |||
374 | Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 | Drug Info | [214] | |||
375 | Tyr-Pro-D-Phe-D-Pro-NH2 | Drug Info | [214] | |||
376 | Tyr-Pro-D-Phe-Pro-NH2 | Drug Info | [214] | |||
377 | Tyr-Pro-D-Phg-Phe-NH2 | Drug Info | [219] | |||
378 | Tyr-Pro-Dmp-Phe-NH2 | Drug Info | [164] | |||
379 | Tyr-Pro-Dmt-Phe-NH2 | Drug Info | [164] | |||
380 | Tyr-Pro-Emp-Phe-NH2 | Drug Info | [164] | |||
381 | Tyr-Pro-Hfe-Phe-NH2 | Drug Info | [219] | |||
382 | Tyr-Pro-Hfe-Pro-NH2 | Drug Info | [219] | |||
383 | Tyr-Pro-Imp-Phe-NH2 | Drug Info | [164] | |||
384 | Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 | Drug Info | [214] | |||
385 | Tyr-Pro-L-(NMe)Phe-Pro-NH2 | Drug Info | [214] | |||
386 | Tyr-Pro-L-Phe-D-Pro-NH2 | Drug Info | [214] | |||
387 | Tyr-Pro-L-Phe-Pro-NH2 | Drug Info | [214] | |||
388 | Tyr-Pro-Mmp-Phe-NH | Drug Info | [164] | |||
389 | Tyr-Pro-Phe-Ala-Bn | Drug Info | [220] | |||
390 | Tyr-Pro-Phe-D-2-Nal-NH2 | Drug Info | [166] | |||
391 | Tyr-Pro-Phe-D-Ala-Bn | Drug Info | [220] | |||
392 | Tyr-Pro-Phe-D-Phg-NH2 | Drug Info | [219] | |||
393 | Tyr-Pro-Phe-D-Val-Bn | Drug Info | [220] | |||
394 | Tyr-Pro-Phe-Hfe-NH2 | Drug Info | [219] | |||
395 | Tyr-Pro-Phe-Phe-N(CH3)2 | Drug Info | [221] | |||
396 | Tyr-Pro-Phe-Phe-NHCH3 | Drug Info | [221] | |||
397 | Tyr-Pro-Phe-Phe-NHNH2 | Drug Info | [221] | |||
398 | Tyr-Pro-Phe-Phe-OC(CH3)3 | Drug Info | [221] | |||
399 | Tyr-Pro-Phe-Phe-OCH2CH3 | Drug Info | [221] | |||
400 | Tyr-Pro-Phe-Phe-OCH2OH | Drug Info | [221] | |||
401 | Tyr-Pro-Phe-Phe-OCH3 | Drug Info | [221] | |||
402 | Tyr-Pro-Phe-Phg-NH2 | Drug Info | [219] | |||
403 | Tyr-Pro-Phg-Phe-NH2 | Drug Info | [219] | |||
404 | Tyr-Pro-Phg-Pro-NH2 | Drug Info | [219] | |||
405 | Tyr-Pro-Tmp-Phe-NH | Drug Info | [164] | |||
406 | Tyr-Pro-Trp-D-Ala-Bn | Drug Info | [220] | |||
407 | Tyr-Pro-Trp-D-Val-Bn | Drug Info | [220] | |||
408 | Tyr-Pro-Trp-Gly-Bn | Drug Info | [220] | |||
409 | Tyr-Sar-Phe-D-2-Nal-NH2 | Drug Info | [166] | |||
410 | UFP-502 | Drug Info | [160] | |||
411 | UFP-512 | Drug Info | [160] | |||
412 | YAWF-NH2 | Drug Info | [140] | |||
413 | YGGWL-NH2 | Drug Info | [140] | |||
414 | YGWFL-NH2 | Drug Info | [140] | |||
415 | YPAA-NH2 | Drug Info | [140] | |||
416 | YPWA-NH2 | Drug Info | [140] | |||
417 | YRFB | Drug Info | [139] | |||
418 | ZYKLOPHIN | Drug Info | [193] | |||
419 | [3H]U69593 | Drug Info | [148] | |||
420 | [D-Ala2]Met-enkephalinamide | Drug Info | [203] | |||
421 | [Dcp1]Dyn A(1-11)-NH2 | Drug Info | [158] | |||
422 | [Leu5]enkephalin | Drug Info | [222] | |||
423 | [Tyr-Pro-Phe-NH-CH2-]2 | Drug Info | [223] | |||
424 | [Tyr-Pro-Phe-NH-]2 | Drug Info | [223] | |||
425 | [Tyr-Pro-Phe-Phe-NH-CH2-]2 | Drug Info | [223] | |||
426 | [Tyr-Pro-Phe-Phe-NH-]2 | Drug Info | [223] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Drug Binding Sites of Target | Top | |||||
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Ligand Name: Morphine | Ligand Info | |||||
Structure Description | Morphine-bound mu-opioid receptor-Gi complex | PDB:8EF6 | ||||
Method | Electron microscopy | Resolution | 3.20 Å | Mutation | No | [224] |
PDB Sequence |
SMITAITIMA
75 LYSIVCVVGL85 FGNFLVMYVI95 VRYTKMKTAT105 NIYIFNLALA115 DALATSTLPF 125 QSVNYLMGTW135 PFGTILCKIV145 ISIDYYNMFT155 SIFTLCTMSV165 DRYIAVCHPV 175 KALDFRTPRN185 AKIINVCNWI195 LSSAIGLPVM205 FMATTKYRQG215 SIDCTLTFSH 225 PTWYWENLLK235 ICVFIFAFIM245 PVLIITVCYG255 LMILRLKSVR265 MLSGSKEKDR 275 NLRRITRMVL285 VVVAVFIVCW295 TPIHIYVIIK305 ALVTIPETTF315 QTVSWHFCIA 325 LGYTNSCLNP335 VLYAFLDENF345 KRCFREF
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Ligand Name: Oliceridine | Ligand Info | |||||
Structure Description | Oliceridine-bound mu-opioid receptor-Gi complex | PDB:8EFB | ||||
Method | Electron microscopy | Resolution | 3.20 Å | Mutation | No | [224] |
PDB Sequence |
TAITIMALYS
78 IVCVVGLFGN88 FLVMYVIVRY98 TKMKTATNIY108 IFNLALADAL118 ATSTLPFQSV 128 NYLMGTWPFG138 TILCKIVISI148 DYYNMFTSIW158 TLCTMSVDRY168 IAVCHPVKAL 178 DFRTPRNAKI188 INVCNWILSS198 AIGLPVMFMA208 TTKYRQGSID218 CTLTFSHPTW 228 YWENLLKICV238 FIFAFIMPVL248 IITVCYGLMI258 LRLKSVRMLS268 GSKEKDRNLR 278 RITRMVLVVV288 AVFIVCWTPI298 HIYVIIKALV308 TIPETTFQTV318 SWHFCIALGY 328 TNSCLNPVLY338 AFLDENFKRC348 FREF
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Click to View More Binding Site Information of This Target with Different Ligands |
Different Human System Profiles of Target | Top |
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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 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 Pathway Affiliation
Biological Network Descriptors
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Estrogen signaling pathway | hsa04915 | Affiliated Target |
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Class: Organismal Systems => Endocrine system | Pathway Hierarchy |
Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 8.62E-05 |
---|---|---|---|---|---|
Closeness centrality | 2.05E-01 | Radiality | 1.36E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 2.07E+01 | Topological coefficient | 3.33E-01 | Eccentricity | 12 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(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 | |||||
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Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | Estrogen signaling pathway | |||||
3 | Morphine addiction | |||||
NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
1 | TCR Signaling Pathway | |||||
Panther Pathway | [+] 3 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
3 | Enkephalin release | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | IL4-mediated signaling events | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Peptide ligand-binding receptors | |||||
2 | G alpha (i) signalling events | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | TCR Signaling Pathway | |||||
2 | GPCRs, Class A Rhodopsin-like | |||||
3 | Peptide GPCRs | |||||
4 | Opioid Signalling | |||||
5 | GPCR ligand binding | |||||
6 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
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