Target Information
| Target General Information | Top | |||||
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| Target ID |
T58992
(Former ID: TTDS00128)
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| Target Name |
Opioid receptor delta (OPRD1)
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| Synonyms |
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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| Gene Name |
OPRD1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Bowel habit change [ICD-11: ME05] | |||||
| 2 | Irritable bowel syndrome [ICD-11: DD91] | |||||
| 3 | Pain [ICD-11: MG30-MG3Z] | |||||
| Function |
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine. G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids.
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC TPSDGPGGGAAA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A03957 ; BADD_A05962 | |||||
| HIT2.0 ID | T42O1D | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Butorphanol | Drug Info | Approved | Pain | [2], [3] | |
| 2 | Codeine | Drug Info | Approved | Pain | [4], [5] | |
| 3 | Eluxadoline | Drug Info | Approved | Diarrhea-predominant irritable bowel syndrome | [6], [7] | |
| 4 | Hydromorphone | Drug Info | Approved | Pain | [8] | |
| 5 | Loperamide | Drug Info | Approved | Diarrhea | [8] | |
| 6 | Oxycodone | Drug Info | Approved | Pain | [9], [10] | |
| Clinical Trial Drug(s) | [+] 10 Clinical Trial Drugs | + | ||||
| 1 | ADL-5747 | Drug Info | Phase 2 | Pain | [11] | |
| 2 | ADL-5859 | Drug Info | Phase 2 | Rheumatoid arthritis | [12] | |
| 3 | AZD-2327 | Drug Info | Phase 2 | Anxiety disorder | [13] | |
| 4 | Met-enkephalin | Drug Info | Phase 2 | Pain | [14], [15] | |
| 5 | TPM-1/Morphine | Drug Info | Phase 2 | Pain | [16] | |
| 6 | AIKO-150 | Drug Info | Phase 1 | Opioid dependence | [17] | |
| 7 | MCP-201 | Drug Info | Phase 1 | Pain | [18] | |
| 8 | MCP-202 | Drug Info | Phase 1 | Overactive bladder | [19] | |
| 9 | SALVINORIN A | Drug Info | Phase 1 | Cerebral vasospasm | [20], [21] | |
| 10 | TRV250 | Drug Info | Phase 1 | Migraine | [21] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | DPI-3290 | Drug Info | Discontinued in Phase 2 | Pain | [22] | |
| 2 | TRK-851 | Drug Info | Discontinued in Phase 1 | Cough | [23] | |
| 3 | VP004 | Drug Info | Discontinued in Phase 1 | Substance use disorder | [24] | |
| 4 | SB-219825 | Drug Info | Terminated | Pain | [28] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | BIO-306 | Drug Info | Preclinical | Migraine | [25] | |
| 2 | LY-25582 | Drug Info | Preclinical | Obesity | [26] | |
| 3 | SoRI-9409 | Drug Info | Preclinical | Alcohol dependence | [27] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Agonist | [+] 38 Agonist drugs | + | ||||
| 1 | Butorphanol | Drug Info | [29] | |||
| 2 | Codeine | Drug Info | [29] | |||
| 3 | Oxycodone | Drug Info | [1] | |||
| 4 | ADL-5747 | Drug Info | [33] | |||
| 5 | ADL-5859 | Drug Info | [33] | |||
| 6 | AZD-2327 | Drug Info | [34] | |||
| 7 | Carfentanil | Drug Info | [35] | |||
| 8 | Met-enkephalin | Drug Info | [36], [37] | |||
| 9 | MCP-201 | Drug Info | [40] | |||
| 10 | MCP-202 | Drug Info | [41] | |||
| 11 | DPI-3290 | Drug Info | [43] | |||
| 12 | BIO-306 | Drug Info | [25] | |||
| 13 | BW 373U86 | Drug Info | [50] | |||
| 14 | 3-Methylfentanyl | Drug Info | [67] | |||
| 15 | 3-Methylthiofentanyl | Drug Info | [68] | |||
| 16 | ARD-412 | Drug Info | [33] | |||
| 17 | BBI-11008 | Drug Info | [33] | |||
| 18 | Beta-endorphin | Drug Info | [83] | |||
| 19 | DADLE | Drug Info | [90], [91] | |||
| 20 | Dihydromorphine | Drug Info | [97] | |||
| 21 | Dimethylthiambutene | Drug Info | [98] | |||
| 22 | DPI-221 | Drug Info | [33] | |||
| 23 | DSLET | Drug Info | [33] | |||
| 24 | DSTBULET | Drug Info | [102] | |||
| 25 | dynorphin B | Drug Info | [33] | |||
| 26 | ethyketazocine | Drug Info | [106] | |||
| 27 | ethylketocyclazocine | Drug Info | [33] | |||
| 28 | Etorphine | Drug Info | [108] | |||
| 29 | Leucine-enkephalin | Drug Info | [133] | |||
| 30 | MCP-203 | Drug Info | [33] | |||
| 31 | MCP-204 | Drug Info | [33] | |||
| 32 | MCP-205 | Drug Info | [33] | |||
| 33 | normorphine | Drug Info | [33] | |||
| 34 | NRP290 | Drug Info | [33] | |||
| 35 | SB 227122 | Drug Info | [148] | |||
| 36 | SNC-80 | Drug Info | [150], [151] | |||
| 37 | Tonazocine mesylate | Drug Info | [151] | |||
| 38 | [3H]diprenorphine | Drug Info | [33] | |||
| Modulator | [+] 3 Modulator drugs | + | ||||
| 1 | Eluxadoline | Drug Info | [30] | |||
| 2 | TRV250 | Drug Info | [21] | |||
| 3 | SB-219825 | Drug Info | [52] | |||
| Binder | [+] 2 Binder drugs | + | ||||
| 1 | Hydromorphone | Drug Info | [31] | |||
| 2 | Loperamide | Drug Info | [32] | |||
| Inhibitor | [+] 347 Inhibitor drugs | + | ||||
| 1 | TPM-1/Morphine | Drug Info | [38] | |||
| 2 | AIKO-150 | Drug Info | [39] | |||
| 3 | SALVINORIN A | Drug Info | [42] | |||
| 4 | Dynorphin a | Drug Info | [44] | |||
| 5 | LY-25582 | Drug Info | [47] | |||
| 6 | BIPHALIN | Drug Info | [49] | |||
| 7 | SB-213698 | Drug Info | [51] | |||
| 8 | SNF-9007 | Drug Info | [53] | |||
| 9 | (-)-cyclorphan | Drug Info | [54] | |||
| 10 | (-)-eseroline | Drug Info | [55] | |||
| 11 | (-)-isoelaeocarpiline | Drug Info | [56] | |||
| 12 | (H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) | Drug Info | [57] | |||
| 13 | 1,10-bis-(Dmt-Tic-amino)decane | Drug Info | [58] | |||
| 14 | 1,4-bis-(Dmt-Tic-amino)butane | Drug Info | [58] | |||
| 15 | 1,6-bis-(Dmt-Tic-amino)hexane | Drug Info | [58] | |||
| 16 | 1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane | Drug Info | [58] | |||
| 17 | 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [59] | |||
| 18 | 1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol | Drug Info | [59] | |||
| 19 | 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol | Drug Info | [59] | |||
| 20 | 1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol | Drug Info | [60] | |||
| 21 | 1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol | Drug Info | [60] | |||
| 22 | 1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol | Drug Info | [60] | |||
| 23 | 1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol | Drug Info | [60] | |||
| 24 | 1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol | Drug Info | [60] | |||
| 25 | 1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol | Drug Info | [60] | |||
| 26 | 1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol | Drug Info | [60] | |||
| 27 | 1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol | Drug Info | [60] | |||
| 28 | 1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol | Drug Info | [60] | |||
| 29 | 1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine | Drug Info | [59] | |||
| 30 | 1-benzhydryl-4-(furan-2-yl)piperidin-4-ol | Drug Info | [60] | |||
| 31 | 1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol | Drug Info | [60] | |||
| 32 | 1-benzhydryl-4-benzylpiperidin-4-ol | Drug Info | [60] | |||
| 33 | 1-benzhydryl-4-butylpiperidin-4-ol | Drug Info | [60] | |||
| 34 | 1-benzhydryl-4-cyclohexylpiperidin-4-ol | Drug Info | [60] | |||
| 35 | 1-benzhydryl-4-ethoxy-4-phenylpiperidine | Drug Info | [59] | |||
| 36 | 1-benzhydryl-4-hexylpiperidin-4-ol | Drug Info | [60] | |||
| 37 | 1-benzhydryl-4-m-tolylpiperidin-4-ol | Drug Info | [60] | |||
| 38 | 1-benzhydryl-4-methoxy-4-phenylpiperidine | Drug Info | [59] | |||
| 39 | 1-benzhydryl-4-o-tolylpiperidin-4-ol | Drug Info | [60] | |||
| 40 | 1-benzhydryl-4-p-tolylpiperidin-4-ol | Drug Info | [60] | |||
| 41 | 1-benzhydryl-4-phenyl-4-propoxypiperidine | Drug Info | [59] | |||
| 42 | 1-benzhydryl-4-phenylpiperidin-4-ol | Drug Info | [61] | |||
| 43 | 1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [62] | |||
| 44 | 1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | [62] | |||
| 45 | 14-O-phenylpropylnaltrexone | Drug Info | [63] | |||
| 46 | 17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [64] | |||
| 47 | 17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine | Drug Info | [64] | |||
| 48 | 17-methyl-4'-methyldihydromorphinone | Drug Info | [65] | |||
| 49 | 17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate | Drug Info | [64] | |||
| 50 | 2-Hydroxymethyl-3-hydroxymorphinan | Drug Info | [64] | |||
| 51 | 3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone | Drug Info | [58] | |||
| 52 | 3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone | Drug Info | [58] | |||
| 53 | 3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone | Drug Info | [58] | |||
| 54 | 3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | Drug Info | [58] | |||
| 55 | 3-desoxy-3-carboxamidonaltrexone | Drug Info | [66] | |||
| 56 | 4-(4-((phenethylamino)methyl)phenoxy)benzamide | Drug Info | [69] | |||
| 57 | 4-(p-Tolyl)spiro[chromene-2,4'-piperidine] | Drug Info | [70] | |||
| 58 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide | Drug Info | [71] | |||
| 59 | 4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol | Drug Info | [70] | |||
| 60 | 4-phenyl-1-(1-phenylbutyl)piperidin-4-ol | Drug Info | [59] | |||
| 61 | 4-phenyl-1-(1-phenylheptyl)piperidin-4-ol | Drug Info | [59] | |||
| 62 | 4-phenyl-1-(1-phenylhexyl)piperidin-4-ol | Drug Info | [59] | |||
| 63 | 4-phenyl-1-(1-phenylpentyl)piperidin-4-ol | Drug Info | [59] | |||
| 64 | 4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol | Drug Info | [59] | |||
| 65 | 4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol | Drug Info | [59] | |||
| 66 | 4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol | Drug Info | [59] | |||
| 67 | 4-phenyl-4-[1H-imidazol-2-yl]-piperidine | Drug Info | [72] | |||
| 68 | 4-Phenylspiro[chromene-2,4'-piperidine] | Drug Info | [70] | |||
| 69 | 5-(4-((phenethylamino)methyl)phenoxy)picolinamide | Drug Info | [69] | |||
| 70 | 6-(2-phenethylisoindolin-5-yloxy)nicotinamide | Drug Info | [73] | |||
| 71 | 6-(4-((benzylamino)methyl)phenoxy)nicotinamide | Drug Info | [69] | |||
| 72 | 6-(4-((phenethylamino)methyl)phenoxy)nicotinamide | Drug Info | [73] | |||
| 73 | 6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide | Drug Info | [73] | |||
| 74 | 6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide | Drug Info | [69] | |||
| 75 | 6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol | Drug Info | [74] | |||
| 76 | 6-cinnamoyl-N-methylstephasunoline | Drug Info | [75] | |||
| 77 | 6-cinnamoylhernandine | Drug Info | [75] | |||
| 78 | 6-desoxonaltrexone | Drug Info | [66] | |||
| 79 | 6beta-naltrexol HCl | Drug Info | [76] | |||
| 80 | 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide | Drug Info | [78] | |||
| 81 | 8-carboxamidocyclazocine | Drug Info | [79] | |||
| 82 | AKNADILACTAM | Drug Info | [75] | |||
| 83 | AMINOFENTANYL | Drug Info | [80] | |||
| 84 | ANALOG OF DYNORPHIN A | Drug Info | [44] | |||
| 85 | Antanal 1 | Drug Info | [81] | |||
| 86 | Antanal 2 | Drug Info | [81] | |||
| 87 | Benzyl derivative of M6G | Drug Info | [82] | |||
| 88 | Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate | Drug Info | [54] | |||
| 89 | BUTORPHAN | Drug Info | [84] | |||
| 90 | CARBOXYFENTANYL | Drug Info | [85] | |||
| 91 | Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [86] | |||
| 92 | Clocinnamox | Drug Info | [63] | |||
| 93 | CTOP | Drug Info | [81] | |||
| 94 | CYCLAZOCINE | Drug Info | [87] | |||
| 95 | CYCLORPHAN | Drug Info | [64] | |||
| 96 | C[L-mTyr-D-pro-L-Phe-D-trp] | Drug Info | [88] | |||
| 97 | C[L-Phe-D-pro-L-mTyr-D-trp] | Drug Info | [88] | |||
| 98 | C[L-Phe-D-pro-L-Phe-L-trp] | Drug Info | [88] | |||
| 99 | D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) | Drug Info | [89] | |||
| 100 | D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) | Drug Info | [89] | |||
| 101 | D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2(CTOP) | Drug Info | [89] | |||
| 102 | D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | [89] | |||
| 103 | DAMGO | Drug Info | [92] | |||
| 104 | Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [93] | |||
| 105 | DELTORPHIN | Drug Info | [94] | |||
| 106 | DELTORPHIN-II | Drug Info | [95] | |||
| 107 | Deprotected cogener of M6G | Drug Info | [82] | |||
| 108 | DERMORPHIN | Drug Info | [96] | |||
| 109 | Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | [93] | |||
| 110 | Dimepheptanol | Drug Info | [74] | |||
| 111 | Dmt-Pro-3,5Dmp-Phe-NH2 | Drug Info | [100] | |||
| 112 | Dmt-Pro-Dmp-Phe-NH2 | Drug Info | [100] | |||
| 113 | Dmt-Pro-Dmt-Phe-NH2 | Drug Info | [100] | |||
| 114 | Dmt-Pro-Emp-Phe-NH2 | Drug Info | [100] | |||
| 115 | Dmt-Pro-Imp-Phe-NH2 | Drug Info | [100] | |||
| 116 | Dmt-Pro-Mmp-Phe-NH2 | Drug Info | [100] | |||
| 117 | Dmt-Pro-Phe-D-1-Nal-NH2 | Drug Info | [101] | |||
| 118 | Dmt-Pro-Phe-D-2-Nal-NH2 | Drug Info | [101] | |||
| 119 | Dmt-Pro-Phe-Phe-NH2 | Drug Info | [100] | |||
| 120 | Dmt-Pro-Tmp-Phe-NH2 | Drug Info | [100] | |||
| 121 | Dmt-Pro-Trp-D-2-Nal-NH2 | Drug Info | [101] | |||
| 122 | DPDPE | Drug Info | [92] | |||
| 123 | ELAEOCARPENINE | Drug Info | [103] | |||
| 124 | ENDOMORPHIN 2 | Drug Info | [104] | |||
| 125 | ENDOMORPHIN-1 | Drug Info | [105] | |||
| 126 | ETONITAZENE | Drug Info | [107] | |||
| 127 | FALCARINDIOL | Drug Info | [109] | |||
| 128 | Grandisine C | Drug Info | [56] | |||
| 129 | Grandisine D | Drug Info | [56] | |||
| 130 | Grandisine F | Drug Info | [56] | |||
| 131 | H-2',6'-dimethyltyrosine-Tic-OH | Drug Info | [110] | |||
| 132 | H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH | Drug Info | [110] | |||
| 133 | H-Aba-ala-Gly-Phe-leu-OH | Drug Info | [37] | |||
| 134 | H-Aba-ala-Gly-Phe-Met-OH | Drug Info | [37] | |||
| 135 | H-Aba-Gly-Gly-Phe-Leu-OH | Drug Info | [37] | |||
| 136 | H-Aba-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [37] | |||
| 137 | H-Apa-ala-Gly-Phe-leu-OH | Drug Info | [37] | |||
| 138 | H-Cdp-ala-Gly-Phe-leu-OH | Drug Info | [37] | |||
| 139 | H-Cdp-Gly-Gly-Phe-Leu-OH | Drug Info | [37] | |||
| 140 | H-Cdp-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [37] | |||
| 141 | H-Cpa-c[pen-Gly-Phe-pen]OH | Drug Info | [37] | |||
| 142 | H-Cpa-Gly-Gly-Phe-Met-NH2 | Drug Info | [37] | |||
| 143 | H-Cpa-Gly-Gly-Phe-Met-OH | Drug Info | [37] | |||
| 144 | H-Cxp-ala-Gly-Phe-leu-OH | Drug Info | [37] | |||
| 145 | H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [111] | |||
| 146 | H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [111] | |||
| 147 | H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | [111] | |||
| 148 | H-Dmt-Aba-Gly-NH-CH2-Bid | Drug Info | [112] | |||
| 149 | H-Dmt-Aba-Gly-NH-CH2-Ph | Drug Info | [112] | |||
| 150 | H-Dmt-Aba-Gly-NH-Ph | Drug Info | [112] | |||
| 151 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 | Drug Info | [113] | |||
| 152 | H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH | Drug Info | [113] | |||
| 153 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 | Drug Info | [114] | |||
| 154 | H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH | Drug Info | [114] | |||
| 155 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 | Drug Info | [114] | |||
| 156 | H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH | Drug Info | [114] | |||
| 157 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 | Drug Info | [114] | |||
| 158 | H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH | Drug Info | [114] | |||
| 159 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 | Drug Info | [114] | |||
| 160 | H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH | Drug Info | [114] | |||
| 161 | H-Dmt-Tic-Asp-N(Me)-Ph | Drug Info | [115] | |||
| 162 | H-Dmt-Tic-Asp-NH-Bzl | Drug Info | [115] | |||
| 163 | H-Dmt-Tic-Asp-NH-Ph | Drug Info | [115] | |||
| 164 | H-Dmt-Tic-D-Asp-N(Me)-Ph | Drug Info | [115] | |||
| 165 | H-Dmt-Tic-D-Asp-NH-Ph | Drug Info | [115] | |||
| 166 | H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) | Drug Info | [57] | |||
| 167 | H-Dmt-Tic-Glu-NH-(CH2)5-NH2 | Drug Info | [116] | |||
| 168 | H-Dmt-Tic-Glu-NH2 | Drug Info | [116] | |||
| 169 | H-Dmt-Tic-Gly-N(Me)-Ph | Drug Info | [115] | |||
| 170 | H-Dmt-Tic-Gly-NH-Bzl | Drug Info | [115] | |||
| 171 | H-Dmt-Tic-Gly-NH-CH2-Bid | Drug Info | [112] | |||
| 172 | H-Dmt-Tic-Gly-NH-Ph | Drug Info | [115] | |||
| 173 | H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph | Drug Info | [117] | |||
| 174 | H-Dmt-Tic-Lys(Ac)-NH-Ph | Drug Info | [117] | |||
| 175 | H-Dmt-Tic-Lys(Z)-NH-CH2-Ph | Drug Info | [117] | |||
| 176 | H-Dmt-Tic-Lys(Z)-NH-Ph | Drug Info | [117] | |||
| 177 | H-Dmt-Tic-Lys-NH-CH2-Ph | Drug Info | [117] | |||
| 178 | H-Dmt-Tic-Lys-NH-Ph | Drug Info | [117] | |||
| 179 | H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H | Drug Info | [118] | |||
| 180 | H-Dmt-Tic-NH-(CH2)6-NH-Phe-H | Drug Info | [118] | |||
| 181 | H-Dmt-Tic-NH-(CH2)6-NH-Tic-H | Drug Info | [118] | |||
| 182 | H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid | Drug Info | [117] | |||
| 183 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid | Drug Info | [115] | |||
| 184 | H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [115] | |||
| 185 | H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | [115] | |||
| 186 | H-Dmt-Tic-NH-CH2-Boa | Drug Info | [119] | |||
| 187 | H-Dmt-Tic-NH-CH2-Bta | Drug Info | [119] | |||
| 188 | H-Dmt-Tic-NH-CH2-CH2-NH2 | Drug Info | [120] | |||
| 189 | H-Dmt-Tic-NH-CH2-Imid | Drug Info | [119] | |||
| 190 | H-Dmt-Tic-NH-CH2-ImidPh | Drug Info | [119] | |||
| 191 | H-Dmt-Tic-NH-CH2-Indl | Drug Info | [119] | |||
| 192 | H-Dmt-Tic-NH-CH2-Indn | Drug Info | [119] | |||
| 193 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid | Drug Info | [117] | |||
| 194 | H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid | Drug Info | [117] | |||
| 195 | H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid | Drug Info | [117] | |||
| 196 | H-mCpa-ala-Gly-Phe-leu-OH | Drug Info | [37] | |||
| 197 | H-mCpa-Gly-Gly-Phe-Leu-OH | Drug Info | [37] | |||
| 198 | H-mCpa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [37] | |||
| 199 | H-Poa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | [37] | |||
| 200 | H-Tyr-c[cys-Gly-Phe(p-NO2)-cys]NH2 | Drug Info | [37] | |||
| 201 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH | Drug Info | [86] | |||
| 202 | H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 | Drug Info | [121] | |||
| 203 | H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 | Drug Info | [121] | |||
| 204 | H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 | Drug Info | [121] | |||
| 205 | H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 | Drug Info | [121] | |||
| 206 | H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 | Drug Info | [122] | |||
| 207 | H-Tyr-c[D-Orn-Aic-Glu]-NH2 | Drug Info | [122] | |||
| 208 | H-Tyr-c[pen-Gly-Phe-pen]OH | Drug Info | [37] | |||
| 209 | H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Drug Info | [123] | |||
| 210 | H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac | Drug Info | [124] | |||
| 211 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H | Drug Info | [125] | |||
| 212 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [125] | |||
| 213 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [125] | |||
| 214 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc | Drug Info | [124] | |||
| 215 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [124] | |||
| 216 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [124] | |||
| 217 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [124] | |||
| 218 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | [125] | |||
| 219 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Drug Info | [123] | |||
| 220 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Drug Info | [123] | |||
| 221 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Drug Info | [123] | |||
| 222 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Drug Info | [123] | |||
| 223 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Drug Info | [123] | |||
| 224 | H-Tyr-Gly-Gly-Phe-Met-NH2 | Drug Info | [37] | |||
| 225 | H-Tyr-NMe-D-Ala-Phe-Sar-NH2 | Drug Info | [126] | |||
| 226 | H-Tyr-Pro-Dap(6DMN)-Phe-NH2 | Drug Info | [57] | |||
| 227 | H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 | Drug Info | [57] | |||
| 228 | H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H | Drug Info | [120] | |||
| 229 | H-Tyr-Tic-Cha-Phe-OH | Drug Info | [114] | |||
| 230 | H-Tyr-Tic-OH | Drug Info | [110] | |||
| 231 | H-Tyr-Tic-Phe-Phe-OH | Drug Info | [114], [127] | |||
| 232 | HERKINORIN | Drug Info | [42] | |||
| 233 | HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 | Drug Info | [128] | |||
| 234 | ICI-174864 | Drug Info | [130] | |||
| 235 | ICI-199441 | Drug Info | [131] | |||
| 236 | Isoelaeocarpine | Drug Info | [132] | |||
| 237 | LOFENTANIL | Drug Info | [134] | |||
| 238 | LONGANINE | Drug Info | [75] | |||
| 239 | Lophocladine a | Drug Info | [135] | |||
| 240 | M6G thiosaccharide analogue | Drug Info | [82] | |||
| 241 | MC-CAM | Drug Info | [136] | |||
| 242 | MCL-117 | Drug Info | [54] | |||
| 243 | MCL-139 | Drug Info | [54] | |||
| 244 | MCL-144 | Drug Info | [137] | |||
| 245 | MCL-145 | Drug Info | [54] | |||
| 246 | MCL-147 | Drug Info | [138] | |||
| 247 | MCL-149 | Drug Info | [138] | |||
| 248 | MCL-153 | Drug Info | [84] | |||
| 249 | MCL-154 | Drug Info | [84] | |||
| 250 | MCL-182 | Drug Info | [138] | |||
| 251 | MCL-183 | Drug Info | [138] | |||
| 252 | MCL-428 | Drug Info | [139] | |||
| 253 | MCL-429 | Drug Info | [139] | |||
| 254 | MCL-431 | Drug Info | [139] | |||
| 255 | MCL-432 | Drug Info | [139] | |||
| 256 | MCL-433 | Drug Info | [139] | |||
| 257 | MCL-434 | Drug Info | [139] | |||
| 258 | MCL-435 | Drug Info | [139] | |||
| 259 | MCL-443 | Drug Info | [139] | |||
| 260 | MCL-444 | Drug Info | [139] | |||
| 261 | MCL-445 | Drug Info | [138] | |||
| 262 | MCL-446 | Drug Info | [138] | |||
| 263 | MCL-447 | Drug Info | [138] | |||
| 264 | MCL-448 | Drug Info | [138] | |||
| 265 | MCL-449 | Drug Info | [139] | |||
| 266 | MCL-450 | Drug Info | [140] | |||
| 267 | MCL-451 | Drug Info | [140] | |||
| 268 | MCL-458 | Drug Info | [138] | |||
| 269 | METAZOCINE | Drug Info | [39] | |||
| 270 | N-(17-Methylmorphinan-3-yl)-N'-phenylurea | Drug Info | [64] | |||
| 271 | N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea | Drug Info | [64] | |||
| 272 | N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 | Drug Info | [141] | |||
| 273 | N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 | Drug Info | [141] | |||
| 274 | N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine | Drug Info | [64] | |||
| 275 | N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine | Drug Info | [64] | |||
| 276 | N-methylstephisoferulin | Drug Info | [75] | |||
| 277 | N-methylstephuline | Drug Info | [75] | |||
| 278 | Naltrexone-6-alpha-ol | Drug Info | [39] | |||
| 279 | NORBINALTORPHIMINE | Drug Info | [144] | |||
| 280 | O-DESMETHYL TRAMADOL | Drug Info | [39] | |||
| 281 | OXYMORPHINDOLE | Drug Info | [145] | |||
| 282 | PERIPENTADENINE | Drug Info | [146] | |||
| 283 | PHENAZOCINE | Drug Info | [39] | |||
| 284 | PROSTEPHABYSSINE | Drug Info | [75] | |||
| 285 | RTI-5989-23 | Drug Info | [47] | |||
| 286 | RTI-5989-25 | Drug Info | [47] | |||
| 287 | RTI-5989-31 | Drug Info | [147] | |||
| 288 | SB-0304 | Drug Info | [126] | |||
| 289 | SN-11 | Drug Info | [51] | |||
| 290 | SN-23 | Drug Info | [51] | |||
| 291 | SN-28 | Drug Info | [149] | |||
| 292 | SOMATOSTATIN | Drug Info | [89] | |||
| 293 | Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | [86] | |||
| 294 | Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 | Drug Info | [153] | |||
| 295 | Tyr-(R)-Aba-Gly-Phe-NH2 | Drug Info | [154] | |||
| 296 | Tyr-(S)-Aba-Gly-Phe-NH2 | Drug Info | [154] | |||
| 297 | Tyr-(S)-spiro-Aba-Gly-Phe-NH2 | Drug Info | [154] | |||
| 298 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 299 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 300 | Tyr-D-Ala-Gly-Phe-Met-NH2 | Drug Info | [49] | |||
| 301 | Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Drug Info | [155] | |||
| 302 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [124] | |||
| 303 | Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 304 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 305 | Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 | Drug Info | [156] | |||
| 306 | Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 | Drug Info | [157] | |||
| 307 | Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 | Drug Info | [156] | |||
| 308 | Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 | Drug Info | [156] | |||
| 309 | Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 | Drug Info | [157] | |||
| 310 | Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 311 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 312 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 313 | Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 314 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 315 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 316 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 317 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 318 | Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 319 | Tyr-Gly-Gly-Phe-c(Cys-Arg-Arg-Ile-Cys)-Arg-lys | Drug Info | [44] | |||
| 320 | Tyr-Gly-Gly-Phe-leu-c(Cys-Arg-Ile-Arg-Cys)-lys | Drug Info | [44] | |||
| 321 | Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 322 | Tyr-Pro-3,5Dmp-Phe-NH2 | Drug Info | [100] | |||
| 323 | Tyr-Pro-D-Phe-D-Pro-NH2 | Drug Info | [153] | |||
| 324 | Tyr-Pro-D-Phe-Pro-NH2 | Drug Info | [153] | |||
| 325 | Tyr-Pro-D-Phg-Phe-NH2 | Drug Info | [158] | |||
| 326 | Tyr-Pro-Dmp-Phe-NH2 | Drug Info | [100] | |||
| 327 | Tyr-Pro-Dmt-Phe-NH2 | Drug Info | [100] | |||
| 328 | Tyr-Pro-Emp-Phe-NH2 | Drug Info | [100] | |||
| 329 | Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [53] | |||
| 330 | Tyr-Pro-Imp-Phe-NH2 | Drug Info | [100] | |||
| 331 | Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 | Drug Info | [153] | |||
| 332 | Tyr-Pro-L-(NMe)Phe-Pro-NH2 | Drug Info | [153] | |||
| 333 | Tyr-Pro-L-Phe-D-Pro-NH2 | Drug Info | [153] | |||
| 334 | Tyr-Pro-L-Phe-Pro-NH2 | Drug Info | [153] | |||
| 335 | Tyr-Pro-Mmp-Phe-NH | Drug Info | [100] | |||
| 336 | Tyr-Pro-Phe-Phe-N(CH3)2 | Drug Info | [159] | |||
| 337 | Tyr-Pro-Phe-Phe-NHCH3 | Drug Info | [159] | |||
| 338 | Tyr-Pro-Phe-Phe-NHNH2 | Drug Info | [159] | |||
| 339 | Tyr-Pro-Phe-Phe-OC(CH3)3 | Drug Info | [159] | |||
| 340 | Tyr-Pro-Phe-Phe-OCH2CH3 | Drug Info | [159] | |||
| 341 | Tyr-Pro-Phe-Phe-OCH2OH | Drug Info | [159] | |||
| 342 | Tyr-Pro-Phe-Phe-OCH3 | Drug Info | [159] | |||
| 343 | Tyr-Pro-Tmp-Phe-NH | Drug Info | [100] | |||
| 344 | UFP-502 | Drug Info | [95] | |||
| 345 | UFP-512 | Drug Info | [95] | |||
| 346 | [Dcp1]Dyn A(1-11)-NH2 | Drug Info | [93] | |||
| 347 | [Leu5]enkephalin | Drug Info | [161] | |||
| Antagonist | [+] 11 Antagonist drugs | + | ||||
| 1 | TRK-851 | Drug Info | [8], [45] | |||
| 2 | SoRI-9409 | Drug Info | [48] | |||
| 3 | 7-benzylidenenaltrexone | Drug Info | [77] | |||
| 4 | CTAP | Drug Info | [33] | |||
| 5 | Diprenorphine | Drug Info | [99] | |||
| 6 | ICI 154129 | Drug Info | [129] | |||
| 7 | naltriben | Drug Info | [142], [143] | |||
| 8 | quadazocine | Drug Info | [33] | |||
| 9 | TIP | Drug Info | [127] | |||
| 10 | TIPPpsi | Drug Info | [152] | |||
| 11 | [3H]naltrindole | Drug Info | [77], [160] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Naltrindole | Ligand Info | |||||
| Structure Description | 1.8 A Structure of the human delta opioid 7TM receptor (PSI Community Target) | PDB:4N6H | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [162] |
| PDB Sequence |
DLEDNWETLN
1011 DNLKVIEKAD1021 NAAQVKDALT1031 KMRAAALDAQ1041 KATPPKLEDK1051 SPDSPEMKDF 1061 RHGFDILVGQ1071 IDDALKLANE1081 GKVKEAQAAA1091 EQLKTTRNAY1101 IQKYLGSPGA 40 RSASSLALAI50 AITALYSAVC60 AVGLLGNVLV70 MFGIVRYTKM80 KTATNIYIFN 90 LALADALATS100 TLPFQSAKYL110 METWPFGELL120 CKAVLSIDYY130 NMFTSIFTLT 140 MMSVDRYIAV150 CHPVKALDFR160 TPAKAKLINI170 CIWVLASGVG180 VPIMVMAVTR 190 PRDGAVVCML200 QFPSPSWYWD210 TVTKICVFLF220 AFVVPILIIT230 VCYGLMLLRL 240 RSVRLLSGSK250 EKDRSLRRIT260 RMVLVVVGAF270 VVCWAPIHIF280 VIVWTLVDID 290 RRDPLVVAAL300 HLCIALGYAN310 SSLNPVLYAF320 LDENFKRCFR330 QLCRKPCG |
|||||
|
|
||||||
| Ligand Name: Oleic acid | Ligand Info | |||||
| Structure Description | 1.8 A Structure of the human delta opioid 7TM receptor (PSI Community Target) | PDB:4N6H | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [162] |
| PDB Sequence |
DLEDNWETLN
1011 DNLKVIEKAD1021 NAAQVKDALT1031 KMRAAALDAQ1041 KATPPKLEDK1051 SPDSPEMKDF 1061 RHGFDILVGQ1071 IDDALKLANE1081 GKVKEAQAAA1091 EQLKTTRNAY1101 IQKYLGSPGA 40 RSASSLALAI50 AITALYSAVC60 AVGLLGNVLV70 MFGIVRYTKM80 KTATNIYIFN 90 LALADALATS100 TLPFQSAKYL110 METWPFGELL120 CKAVLSIDYY130 NMFTSIFTLT 140 MMSVDRYIAV150 CHPVKALDFR160 TPAKAKLINI170 CIWVLASGVG180 VPIMVMAVTR 190 PRDGAVVCML200 QFPSPSWYWD210 TVTKICVFLF220 AFVVPILIIT230 VCYGLMLLRL 240 RSVRLLSGSK250 EKDRSLRRIT260 RMVLVVVGAF270 VVCWAPIHIF280 VIVWTLVDID 290 RRDPLVVAAL300 HLCIALGYAN310 SSLNPVLYAF320 LDENFKRCFR330 QLCRKPCG |
|||||
|
|
ALA47
3.594
LEU48
3.835
ILE50
4.281
ALA51
3.883
ALA54
3.583
LEU55
3.528
ALA58
3.811
CYS60
4.375
LEU64
4.150
MET71
3.997
PHE72
3.842
VAL75
3.839
ALA83
4.516
TYR87
2.568
PHE89
4.231
LEU93
4.063
ALA96
3.956
LEU97
4.130
SER100
3.372
THR101
4.491
PRO103
3.757
PHE104
4.051
ALA107
4.212
PRO115
3.024
PHE116
3.347
GLY117
4.037
LEU120
4.504
VAL124
4.931
ILE127
4.078
MET141
3.957
VAL144
4.649
ASP145
2.709
ILE148
3.895
PHE159
3.301
ARG160
3.823
THR161
3.646
LYS164
3.891
ALA165
3.780
ILE168
3.717
TYR233
3.250
LEU237
3.726
ARG261
3.328
LEU264
4.076
VAL265
4.119
GLY268
3.886
ALA269
3.951
VAL271
4.172
VAL272
3.653
CYS273
4.017
ALA275
4.362
PRO276
3.737
ILE279
3.637
PHE280
3.952
VAL283
4.095
VAL287
3.710
ASP288
3.451
ILE289
3.612
ASP290
2.702
ASP293
3.174
LEU295
3.387
VAL296
3.543
ALA298
4.577
ALA299
4.120
LEU302
4.246
CYS303
4.234
LEU306
3.926
ALA309
4.042
LEU313
3.725
VAL316
3.694
LEU317
4.280
PHE320
3.506
LEU321
3.874
|
|||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| 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 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).
Human Similarity Proteins
Human Pathway Affiliation
|
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| cGMP-PKG signaling pathway | hsa04022 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Sphingolipid signaling pathway | hsa04071 | 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 | ||
| 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 | |
|
|
||
| "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-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | cGMP-PKG signaling pathway | |||||
| 2 | Sphingolipid signaling pathway | |||||
| 3 | Neuroactive ligand-receptor interaction | |||||
| Panther Pathway | [+] 5 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 | |||||
| 4 | Opioid proenkephalin pathway | |||||
| 5 | Opioid proopiomelanocortin pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Peptide GPCRs | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Oxycodone: a pharmacological and clinical review. Clin Transl Oncol. 2007 May;9(5):298-307. | |||||
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