Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T58992 | ||||
Target Name | Opioid receptor delta (OPRD1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Butorphanol | Drug Info | Ki = 0.5 nM | [91] | |
Codeine | Drug Info | Ki > 1000 nM | |||
Hydrocodone | Drug Info | Ki = 1021 nM | |||
Loperamide | Drug Info | IC50 = 6.9 nM | [92] | ||
Nalbuphine | Drug Info | Ki = 1.4 nM | [91] | ||
BIO-306 | Drug Info | IC50 = 130 nM | [93] | ||
Drug Info | Ki = 70 nM | [2] | |||
Drug Info | IC50 = 6.9 nM | [62] | |||
(-)-cyclorphan | Drug Info | Ki = 1.9 nM | [10] | ||
(-)-eseroline | Drug Info | IC50 = 10000 nM | |||
(-)-isoelaeocarpiline | Drug Info | IC50 = 9900 nM | [24] | ||
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) | Drug Info | Ki = 0.158 nM | [15] | ||
1,10-bis-(Dmt-Tic-amino)decane | Drug Info | Ki = 1.53 nM | [8] | ||
1,4-bis-(Dmt-Tic-amino)butane | Drug Info | Ki = 0.124 nM | [8] | ||
1,6-bis-(Dmt-Tic-amino)hexane | Drug Info | Ki = 0.129 nM | [8] | ||
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol | Drug Info | Ki = 187 nM | [33] | ||
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol | Drug Info | Ki = 15250 nM | [33] | ||
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol | Drug Info | Ki = 5791 nM | [33] | ||
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol | Drug Info | Ki = 5610 nM | [32] | ||
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol | Drug Info | Ki = 4392 nM | [32] | ||
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol | Drug Info | Ki = 5610 nM | [32] | ||
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol | Drug Info | Ki = 9585 nM | [32] | ||
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol | Drug Info | Ki = 13750 nM | [32] | ||
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol | Drug Info | Ki = 15240 nM | [32] | ||
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol | Drug Info | Ki = 6364 nM | [32] | ||
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol | Drug Info | Ki = 3325 nM | [32] | ||
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol | Drug Info | Ki = 19220 nM | [32] | ||
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine | Drug Info | Ki = 3741 nM | [33] | ||
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol | Drug Info | Ki = 14455 nM | [32] | ||
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol | Drug Info | Ki = 8446 nM | [32] | ||
1-benzhydryl-4-benzylpiperidin-4-ol | Drug Info | Ki = 15010 nM | [32] | ||
1-benzhydryl-4-butylpiperidin-4-ol | Drug Info | Ki = 18800 nM | [32] | ||
1-benzhydryl-4-cyclohexylpiperidin-4-ol | Drug Info | Ki = 8105 nM | [32] | ||
1-benzhydryl-4-ethoxy-4-phenylpiperidine | Drug Info | Ki = 898 nM | [33] | ||
1-benzhydryl-4-hexylpiperidin-4-ol | Drug Info | Ki = 17865 nM | [32] | ||
1-benzhydryl-4-m-tolylpiperidin-4-ol | Drug Info | Ki = 7796 nM | [32] | ||
1-benzhydryl-4-methoxy-4-phenylpiperidine | Drug Info | Ki = 2651 nM | [33] | ||
1-benzhydryl-4-o-tolylpiperidin-4-ol | Drug Info | Ki = 1668 nM | [32] | ||
1-benzhydryl-4-p-tolylpiperidin-4-ol | Drug Info | Ki = 12115 nM | [32] | ||
1-benzhydryl-4-phenyl-4-propoxypiperidine | Drug Info | Ki = 2767 nM | [33] | ||
1-benzhydryl-4-phenylpiperidin-4-ol | Drug Info | Ki = 1666 nM | [63] | ||
1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Drug Info | Ki = 1500 nM | [17] | ||
14-O-phenylpropylnaltrexone | Drug Info | Ki = 0.48 nM | [61] | ||
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine | Drug Info | Ki = 39 nM | [73] | ||
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine | Drug Info | Ki = 5.4 nM | [73] | ||
17-methyl-4'-methyldihydromorphinone | Drug Info | Ki = 4 nM | [19] | ||
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate | Drug Info | Ki = 160 nM | [73] | ||
2-Hydroxymethyl-3-hydroxymorphinan | Drug Info | Ki = 1400 nM | [73] | ||
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone | Drug Info | Ki = 0.323 nM | [8] | ||
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone | Drug Info | Ki = 0.163 nM | [8] | ||
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | Drug Info | Ki = 0.155 nM | [8] | ||
3-desoxy-3-carboxamidonaltrexone | Drug Info | Ki = 550 nM | [62] | ||
4-(4-((phenethylamino)methyl)phenoxy)benzamide | Drug Info | Ki = 1.88 nM | [40] | ||
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] | Drug Info | Ki = 72 nM | [56] | ||
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide | Drug Info | Ki = 17 nM | [68] | ||
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol | Drug Info | Ki = 59 nM | [56] | ||
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol | Drug Info | Ki = 4126 nM | [33] | ||
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol | Drug Info | Ki = 550 nM | [33] | ||
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol | Drug Info | Ki = 184 nM | [33] | ||
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol | Drug Info | Ki = 441 nM | [33] | ||
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol | Drug Info | Ki = 2437 nM | [33] | ||
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol | Drug Info | Ki = 9365 nM | [33] | ||
4-phenyl-4-[1H-imidazol-2-yl]-piperidine | Drug Info | Ki = 81 nM | [7] | ||
4-Phenylspiro[chromene-2,4'-piperidine] | Drug Info | Ki = 71 nM | [56] | ||
5-(4-((phenethylamino)methyl)phenoxy)picolinamide | Drug Info | Ki = 8.54 nM | [40] | ||
6-(2-phenethylisoindolin-5-yloxy)nicotinamide | Drug Info | Ki = 2274 nM | [43] | ||
6-(4-((benzylamino)methyl)phenoxy)nicotinamide | Drug Info | Ki = 54.15 nM | [40] | ||
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide | Drug Info | Ki = 1.16 nM | [43] | ||
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide | Drug Info | Ki = 70.21 nM | [43] | ||
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide | Drug Info | Ki = 495.99 nM | [40] | ||
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol | Drug Info | Ki = 150 nM | [84] | ||
6-cinnamoyl-N-methylstephasunoline | Drug Info | IC50 = 11300 nM | [77] | ||
6-cinnamoylhernandine | Drug Info | IC50 = 5100 nM | [77] | ||
6-desoxonaltrexone | Drug Info | Ki = 79 nM | [62] | ||
6beta-naltrexol HCl | Drug Info | Ki = 213 nM | [65] | ||
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide | Drug Info | IC50 = 8306 nM | [80] | ||
8-carboxamidocyclazocine | Drug Info | Ki = 5.2 nM | [52] | ||
AIKO-150 | Drug Info | Ki = 53 nM | [59] | ||
AKNADILACTAM | Drug Info | IC50 = 17000 nM | [77] | ||
AMINOFENTANYL | Drug Info | IC50 = 13000 nM | [18] | ||
ANALOG OF DYNORPHIN A | Drug Info | IC50 = 9.1 nM | [86] | ||
Antanal 1 | Drug Info | Ki = 17.4 nM | [57] | ||
Antanal 2 | Drug Info | Ki = 7.74 nM | [57] | ||
Benzyl derivative of M6G | Drug Info | Ki = 7.2 nM | [4] | ||
BIPHALIN | Drug Info | IC50 = 2.7 nM | [69] | ||
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate | Drug Info | Ki = 190 nM | [10] | ||
BUTORPHAN | Drug Info | Ki = 5.9 nM | [75] | ||
CARBOXYFENTANYL | Drug Info | Ki = 9400 nM | [42] | ||
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | IC50 = 0.59 nM | [38] | ||
Clocinnamox | Drug Info | Ki = 2.7 nM | [61] | ||
CTOP | Drug Info | IC50 = 13500 nM | [57] | ||
CYCLAZOCINE | Drug Info | Ki = 2 nM | [60] | ||
CYCLORPHAN | Drug Info | Ki = 1.9 nM | [73] | ||
C[L-mTyr-D-pro-L-Phe-D-trp] | Drug Info | Ki = 670 nM | [66] | ||
C[L-Phe-D-pro-L-mTyr-D-trp] | Drug Info | Ki = 3400 nM | [66] | ||
C[L-Phe-D-pro-L-Phe-L-trp] | Drug Info | Ki = 2000 nM | [66] | ||
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) | Drug Info | IC50 = 4500 nM | [83] | ||
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) | Drug Info | IC50 = 8400 nM | [83] | ||
D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2(CTOP) | Drug Info | IC50 = 13500 nM | [83] | ||
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 | Drug Info | IC50 = 2800 nM | [83] | ||
DADLE | Drug Info | IC50 = 0.27 nM | [37] | ||
DAMGO | Drug Info | Ki = 2670 nM | |||
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | Ki = 25.8 nM | [20] | ||
DELTORPHIN-II | Drug Info | IC50 = 0.53 nM | [78] | ||
Deprotected cogener of M6G | Drug Info | Ki = 266.3 nM | [4] | ||
DERMORPHIN | Drug Info | IC50 = 15.2 nM | [9] | ||
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Drug Info | Ki = 11.6 nM | [20] | ||
Dimepheptanol | Drug Info | Ki = 230 nM | [84] | ||
Dmt-Pro-3,5Dmp-Phe-NH2 | Drug Info | Ki = 11.6 nM | [36] | ||
Dmt-Pro-Dmp-Phe-NH2 | Drug Info | Ki = 2.27 nM | [36] | ||
Dmt-Pro-Dmt-Phe-NH2 | Drug Info | Ki = 80.8 nM | [36] | ||
Dmt-Pro-Emp-Phe-NH2 | Drug Info | IC50 = 0.51 nM | [36] | ||
Dmt-Pro-Imp-Phe-NH2 | Drug Info | IC50 = 5.56 nM | [36] | ||
Dmt-Pro-Mmp-Phe-NH2 | Drug Info | Ki = 4.61 nM | [36] | ||
Dmt-Pro-Phe-D-1-Nal-NH2 | Drug Info | Ki = 27.1 nM | [28] | ||
Dmt-Pro-Phe-D-2-Nal-NH2 | Drug Info | Ki = 7.74 nM | [28] | ||
Dmt-Pro-Phe-Phe-NH2 | Drug Info | IC50 = 0.59 nM | [36] | ||
Dmt-Pro-Tmp-Phe-NH2 | Drug Info | Ki = 1.83 nM | [36] | ||
Dmt-Pro-Trp-D-2-Nal-NH2 | Drug Info | Ki = 17.4 nM | [28] | ||
DPDPE | Drug Info | Ki = 2.72 nM | |||
ELAEOCARPENINE | Drug Info | Ki = 14000 nM | [74] | ||
ENDOMORPHIN 2 | Drug Info | IC50 = 510 nM | [79] | ||
ENDOMORPHIN-1 | Drug Info | Ki = 1909 nM | [54] | ||
ETONITAZENE | Drug Info | Ki = 0.6 nM | [82] | ||
FALCARINDIOL | Drug Info | Ki = 1096 nM | [46] | ||
Grandisine C | Drug Info | IC50 = 14600 nM | [24] | ||
Grandisine D | Drug Info | IC50 = 1650 nM | [24] | ||
Grandisine F | Drug Info | IC50 = 1550 nM | [24] | ||
H-2',6'-dimethyltyrosine-Tic-OH | Drug Info | Ki = 1.84 nM | [71] | ||
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH | Drug Info | Ki = 0.248 nM | [71] | ||
H-Aba-ala-Gly-Phe-leu-OH | Drug Info | Ki = 10 nM | [31] | ||
H-Aba-ala-Gly-Phe-Met-OH | Drug Info | Ki = 1 nM | [31] | ||
H-Aba-Gly-Gly-Phe-Leu-OH | Drug Info | Ki = 19 nM | [31] | ||
H-Aba-ser-Gly-Phe-Leu-Thr-OH | Drug Info | Ki = 3.8 nM | [31] | ||
H-Apa-ala-Gly-Phe-leu-OH | Drug Info | Ki = 19 nM | [31] | ||
H-Cdp-ala-Gly-Phe-leu-OH | Drug Info | Ki = 0.78 nM | [31] | ||
H-Cdp-Gly-Gly-Phe-Leu-OH | Drug Info | Ki = 1 nM | [31] | ||
H-Cdp-ser-Gly-Phe-Leu-Thr-OH | Drug Info | Ki = 1.2 nM | [31] | ||
H-Cpa-c[pen-Gly-Phe-pen]OH | Drug Info | Ki = 19 nM | [31] | ||
H-Cpa-Gly-Gly-Phe-Met-NH2 | Drug Info | Ki = 1.3 nM | [31] | ||
H-Cpa-Gly-Gly-Phe-Met-OH | Drug Info | Ki = 1.8 nM | [31] | ||
H-Cxp-ala-Gly-Phe-leu-OH | Drug Info | Ki = 1100 nM | [31] | ||
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | IC50 = 211 nM | [1] | ||
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | IC50 = 1270 nM | [1] | ||
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Drug Info | IC50 = 3530 nM | [1] | ||
H-Dmt-Aba-Gly-NH-CH2-Bid | Drug Info | IC50 = 2700 nM | [16] | ||
H-Dmt-Aba-Gly-NH-CH2-Ph | Drug Info | IC50 = 830 nM | [16] | ||
H-Dmt-Aba-Gly-NH-Ph | Drug Info | IC50 = 650 nM | [16] | ||
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 | Drug Info | IC50 = 1.69 nM | [5] | ||
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH | Drug Info | IC50 = 682 nM | [5] | ||
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 | Drug Info | Ki = 13 nM | [27] | ||
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH | Drug Info | Ki = 2 nM | [27] | ||
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 | Drug Info | Ki = 7 nM | [27] | ||
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH | Drug Info | Ki = 1.5 nM | [27] | ||
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 | Drug Info | Ki = 4.1 nM | [27] | ||
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH | Drug Info | Ki = 2 nM | [27] | ||
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 | Drug Info | Ki = 4 nM | [27] | ||
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH | Drug Info | Ki = 0.48 nM | [27] | ||
H-Dmt-Tic-Asp-N(Me)-Ph | Drug Info | Ki = 0.186 nM | [55] | ||
H-Dmt-Tic-Asp-NH-Ph | Drug Info | IC50 = 265 nM | [55] | ||
H-Dmt-Tic-D-Asp-NH-Ph | Drug Info | IC50 = 2655 nM | [55] | ||
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) | Drug Info | Ki = 7.8 nM | [15] | ||
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 | Drug Info | Ki = 0.22 nM | [3] | ||
H-Dmt-Tic-Glu-NH2 | Drug Info | IC50 = 2.58 nM | [3] | ||
H-Dmt-Tic-Gly-N(Me)-Ph | Drug Info | IC50 = 1466 nM | [55] | ||
H-Dmt-Tic-Gly-NH-Bzl | Drug Info | IC50 = 2.69 nM | [55] | ||
H-Dmt-Tic-Gly-NH-CH2-Bid | Drug Info | IC50 = 0.13 nM | [16] | ||
H-Dmt-Tic-Gly-NH-Ph | Drug Info | IC50 = 2.57 nM | [55] | ||
H-Dmt-Tic-Lys(Ac)-NH-Ph | Drug Info | Ki = 0.13 nM | [22] | ||
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph | Drug Info | Ki = 0.31 nM | [22] | ||
H-Dmt-Tic-Lys(Z)-NH-Ph | Drug Info | Ki = 0.57 nM | [22] | ||
H-Dmt-Tic-Lys-NH-CH2-Ph | Drug Info | Ki = 0.5 nM | [22] | ||
H-Dmt-Tic-Lys-NH-Ph | Drug Info | Ki = 0.42 nM | [22] | ||
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H | Drug Info | Ki = 0.23 nM | [6] | ||
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H | Drug Info | Ki = 0.89 nM | [6] | ||
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H | Drug Info | Ki = 0.13 nM | [6] | ||
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid | Drug Info | Ki = 0.4 nM | [22] | ||
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid | Drug Info | IC50 = 179 nM | [55] | ||
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) | Drug Info | IC50 = 2886 nM | [55] | ||
H-Dmt-Tic-NH-CH2-Boa | Drug Info | Ki = 0.283 nM | [47] | ||
H-Dmt-Tic-NH-CH2-Bta | Drug Info | Ki = 0.145 nM | [47] | ||
H-Dmt-Tic-NH-CH2-CH2-NH2 | Drug Info | Ki = 1.81 nM | [41] | ||
H-Dmt-Tic-NH-CH2-Imid | Drug Info | IC50 = 3.63 nM | [47] | ||
H-Dmt-Tic-NH-CH2-ImidPh | Drug Info | Ki = 0.443 nM | [47] | ||
H-Dmt-Tic-NH-CH2-Indn | Drug Info | IC50 = 129 nM | [47] | ||
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid | Drug Info | Ki = 0.18 nM | [22] | ||
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid | Drug Info | IC50 = 9049 nM | [22] | ||
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid | Drug Info | Ki = 0.49 nM | [22] | ||
H-mCpa-ala-Gly-Phe-leu-OH | Drug Info | Ki = 170 nM | [31] | ||
H-mCpa-Gly-Gly-Phe-Leu-OH | Drug Info | Ki = 475 nM | [31] | ||
H-mCpa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | Ki = 42 nM | [31] | ||
H-Poa-ser-Gly-Phe-Leu-Thr-OH | Drug Info | Ki = 360 nM | [31] | ||
H-Tyr-c[cys-Gly-Phe(p-NO2)-cys]NH2 | Drug Info | IC50 = 0.232 nM | [31] | ||
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH | Drug Info | IC50 = 3.4 nM | [38] | ||
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 | Drug Info | Ki = 0.822 nM | [30] | ||
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 | Drug Info | Ki = 1.61 nM | [30] | ||
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 | Drug Info | Ki = 3510 nM | [12] | ||
H-Tyr-c[D-Orn-Aic-Glu]-NH2 | Drug Info | Ki = 209 nM | [12] | ||
H-Tyr-c[pen-Gly-Phe-pen]OH | Drug Info | Ki = 3.2 nM | [31] | ||
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Drug Info | IC50 = 400 nM | [48] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac | Drug Info | IC50 = 5.1 nM | [11] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H | Drug Info | IC50 = 15 nM | [26] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | IC50 = 16 nM | [26] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | IC50 = 12 nM | [26] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc | Drug Info | IC50 = 24 nM | [11] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | IC50 = 26 nM | [11] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | IC50 = 36 nM | [11] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | IC50 = 230 nM | [11] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | IC50 = 25 nM | [26] | ||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Drug Info | IC50 = 45 nM | [48] | ||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Drug Info | IC50 = 50 nM | [48] | ||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Drug Info | IC50 = 150 nM | [48] | ||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Drug Info | IC50 = 41 nM | [48] | ||
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Drug Info | IC50 = 40 nM | [48] | ||
H-Tyr-Gly-Gly-Phe-Met-NH2 | Drug Info | Ki = 10 nM | [31] | ||
H-Tyr-NMe-D-Ala-Phe-Sar-NH2 | Drug Info | IC50 = 7100 nM | [49] | ||
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 | Drug Info | IC50 = 500 nM | [15] | ||
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 | Drug Info | IC50 = 300 nM | [15] | ||
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H | Drug Info | Ki = 1.45 nM | [41] | ||
H-Tyr-Tic-Cha-Phe-OH | Drug Info | Ki = 0.61 nM | [27] | ||
H-Tyr-Tic-OH | Drug Info | Ki = 242 nM | [71] | ||
HERKINORIN | Drug Info | Ki = 1170 nM | [50] | ||
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 | Drug Info | Ki = 6.18 nM | [70] | ||
ICI-174864 | Drug Info | IC50 = 83 nM | [21] | ||
Isoelaeocarpine | Drug Info | IC50 = 13600 nM | [35] | ||
LOFENTANIL | Drug Info | IC50 = 0.25 nM | [85] | ||
LONGANINE | Drug Info | IC50 = 700 nM | [77] | ||
LY-25582 | Drug Info | Ki = 198 nM | [90] | ||
M6G thiosaccharide analogue | Drug Info | Ki = 31.4 nM | [4] | ||
MC-CAM | Drug Info | Ki = 4.79 nM | [72] | ||
MCL-117 | Drug Info | Ki = 0.62 nM | [10] | ||
MCL-139 | Drug Info | Ki = 9.4 nM | [10] | ||
MCL-144 | Drug Info | Ki = 4.2 nM | [67] | ||
MCL-145 | Drug Info | Ki = 9.4 nM | [10] | ||
MCL-147 | Drug Info | Ki = 29 nM | [34] | ||
MCL-149 | Drug Info | Ki = 150 nM | [34] | ||
MCL-153 | Drug Info | Ki = 730 nM | [75] | ||
MCL-154 | Drug Info | Ki = 2500 nM | [75] | ||
MCL-182 | Drug Info | Ki = 180 nM | [34] | ||
MCL-183 | Drug Info | Ki = 230 nM | [34] | ||
MCL-428 | Drug Info | Ki = 3.9 nM | [29] | ||
MCL-429 | Drug Info | Ki = 1.6 nM | [29] | ||
MCL-431 | Drug Info | Ki = 78 nM | [29] | ||
MCL-432 | Drug Info | Ki = 27 nM | [29] | ||
MCL-433 | Drug Info | Ki = 53 nM | [29] | ||
MCL-434 | Drug Info | Ki = 42 nM | [29] | ||
MCL-435 | Drug Info | Ki = 30 nM | [29] | ||
MCL-443 | Drug Info | Ki = 15 nM | [29] | ||
MCL-444 | Drug Info | Ki = 2.7 nM | [29] | ||
MCL-445 | Drug Info | Ki = 270 nM | [34] | ||
MCL-446 | Drug Info | Ki = 50 nM | [34] | ||
MCL-447 | Drug Info | Ki = 160 nM | [34] | ||
MCL-448 | Drug Info | Ki = 23 nM | [34] | ||
MCL-449 | Drug Info | Ki = 2.8 nM | [29] | ||
MCL-450 | Drug Info | IC50 = 3.9 nM | [23] | ||
MCL-451 | Drug Info | IC50 = 10 nM | [23] | ||
MCL-458 | Drug Info | Ki = 360 nM | [34] | ||
Met-enkephalin | Drug Info | Ki = 2 nM | [31] | ||
METAZOCINE | Drug Info | Ki = 140 nM | [59] | ||
N-(17-Methylmorphinan-3-yl)-N'-phenylurea | Drug Info | Ki = 320 nM | [73] | ||
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea | Drug Info | Ki = 300 nM | [73] | ||
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 | Drug Info | IC50 = 1288 nM | [25] | ||
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 | Drug Info | IC50 = 1343 nM | [25] | ||
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine | Drug Info | Ki = 130 nM | [73] | ||
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine | Drug Info | Ki = 29 nM | [73] | ||
N-methylstephisoferulin | Drug Info | IC50 = 2500 nM | [77] | ||
N-methylstephuline | Drug Info | IC50 = 2100 nM | [77] | ||
Naltrexone-6-alpha-ol | Drug Info | Ki = 56 nM | [59] | ||
NORBINALTORPHIMINE | Drug Info | Ki = 86 nM | [2] | ||
O-DESMETHYL TRAMADOL | Drug Info | Ki = 2900 nM | [59] | ||
OXYMORPHINDOLE | Drug Info | Ki = 0.8 nM | [51] | ||
PERIPENTADENINE | Drug Info | IC50 = 11400 nM | [44] | ||
PHENAZOCINE | Drug Info | Ki = 5 nM | [59] | ||
PROSTEPHABYSSINE | Drug Info | IC50 = 5500 nM | [77] | ||
RTI-5989-23 | Drug Info | Ki = 168 nM | [90] | ||
RTI-5989-25 | Drug Info | Ki = 142 nM | [90] | ||
RTI-5989-31 | Drug Info | Ki = 270 nM | [39] | ||
SALVINORIN A | Drug Info | Ki = 3990 nM | [50] | ||
SB-0304 | Drug Info | IC50 = 17800 nM | [49] | ||
SB-213698 | Drug Info | Ki = 1.44 nM | [64] | ||
SN-11 | Drug Info | Ki = 0.19 nM | [64] | ||
SN-23 | Drug Info | Ki = 0.19 nM | [64] | ||
SN-28 | Drug Info | Ki = 0.14 nM | [81] | ||
SNF-9007 | Drug Info | IC50 = 29 nM | [14] | ||
SOMATOSTATIN | Drug Info | IC50 = 2000 nM | [83] | ||
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Drug Info | IC50 = 0.76 nM | [38] | ||
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 | Drug Info | IC50 = 202 nM | [88] | ||
Tyr-(R)-Aba-Gly-Phe-NH2 | Drug Info | Ki = 2.965 nM | [45] | ||
Tyr-(S)-Aba-Gly-Phe-NH2 | Drug Info | Ki = 0.778 nM | [45] | ||
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 | Drug Info | Ki = 2.312 nM | [45] | ||
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 1300 nM | [14] | ||
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 63 nM | [14] | ||
Tyr-D-Ala-Gly-Phe-Met-NH2 | Drug Info | IC50 = 36 nM | [69] | ||
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Drug Info | IC50 = 4.8 nM | [58] | ||
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | IC50 = 42 nM | [11] | ||
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 45 nM | [14] | ||
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 66 nM | [14] | ||
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 | Drug Info | Ki = 1.55 nM | [89] | ||
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 | Drug Info | IC50 = 0.67 nM | [87] | ||
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 | Drug Info | Ki = 67 nM | [89] | ||
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 | Drug Info | Ki = 1760 nM | [89] | ||
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 | Drug Info | IC50 = 0.28 nM | [87] | ||
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 310 nM | [14] | ||
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 700 nM | [14] | ||
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 23 nM | [14] | ||
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 9 nM | [14] | ||
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 170 nM | [14] | ||
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 24 nM | [14] | ||
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | IC50 = 12 nM | [14] | ||
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 65 nM | [14] | ||
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 890 nM | [14] | ||
Tyr-Gly-Gly-Phe-c(Cys-Arg-Arg-Ile-Cys)-Arg-lys | Drug Info | IC50 = 6262 nM | [86] | ||
Tyr-Gly-Gly-Phe-leu-c(Cys-Arg-Ile-Arg-Cys)-lys | Drug Info | IC50 = 92.6 nM | [86] | ||
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | IC50 = 220 nM | [14] | ||
Tyr-Pro-3,5Dmp-Phe-NH2 | Drug Info | Ki = 3451 nM | [36] | ||
Tyr-Pro-D-Phe-D-Pro-NH2 | Drug Info | IC50 = 4810 nM | [88] | ||
Tyr-Pro-D-Phe-Pro-NH2 | Drug Info | IC50 = 594 nM | [88] | ||
Tyr-Pro-D-Phg-Phe-NH2 | Drug Info | Ki = 2100 nM | [13] | ||
Tyr-Pro-Dmp-Phe-NH2 | Drug Info | IC50 = 1.39 nM | [36] | ||
Tyr-Pro-Dmt-Phe-NH2 | Drug Info | IC50 = 978 nM | [36] | ||
Tyr-Pro-Emp-Phe-NH2 | Drug Info | IC50 = 277 nM | [36] | ||
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 1500 nM | [14] | ||
Tyr-Pro-Imp-Phe-NH2 | Drug Info | Ki = 543 nM | [36] | ||
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 | Drug Info | IC50 = 1250 nM | [88] | ||
Tyr-Pro-L-(NMe)Phe-Pro-NH2 | Drug Info | IC50 = 1790 nM | [88] | ||
Tyr-Pro-L-Phe-D-Pro-NH2 | Drug Info | IC50 = 1508 nM | [88] | ||
Tyr-Pro-L-Phe-Pro-NH2 | Drug Info | IC50 = 3690 nM | [88] | ||
Tyr-Pro-Mmp-Phe-NH | Drug Info | IC50 = 15.7 nM | [36] | ||
Tyr-Pro-Phe-Phe-N(CH3)2 | Drug Info | IC50 = 2723 nM | [53] | ||
Tyr-Pro-Phe-Phe-NHCH3 | Drug Info | Ki = 8474 nM | [53] | ||
Tyr-Pro-Phe-Phe-NHNH2 | Drug Info | IC50 = 185 nM | [53] | ||
Tyr-Pro-Phe-Phe-OC(CH3)3 | Drug Info | Ki = 247 nM | [53] | ||
Tyr-Pro-Phe-Phe-OCH2CH3 | Drug Info | Ki = 2940 nM | [53] | ||
Tyr-Pro-Phe-Phe-OCH2OH | Drug Info | IC50 = 29.17 nM | [53] | ||
Tyr-Pro-Phe-Phe-OCH3 | Drug Info | IC50 = 37.2 nM | [53] | ||
Tyr-Pro-Tmp-Phe-NH | Drug Info | Ki = 1358 nM | [36] | ||
UFP-502 | Drug Info | IC50 = 0.13 nM | [78] | ||
UFP-512 | Drug Info | IC50 = 0.12 nM | [78] | ||
[Dcp1]Dyn A(1-11)-NH2 | Drug Info | Ki = 129 nM | [20] | ||
[Leu5]enkephalin | Drug Info | Ki = 2.53 nM | [76] | ||
Action against Disease Model | Butorphanol | Drug Info | HEK-delta Cells IC50: 61 nM | ||
Hydromorphone | Drug Info | HEK-deltaCells IC50: 54 nM | |||
Nalbuphine | Drug Info | HEK-delta Cells IC50: 545 nM | |||
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