Target Validation Information
TTD ID T47768
Target Name Opioid receptor mu (MOP)
Type of Target
Successful
Drug Potency against Target Alvimopan Drug Info Ki = 0.44 nM
Naloxone Drug Info IC50 = 7.6 nM [110]
Remifentanil Drug Info EC50 = 5.69 nM [111]
Drug Info Ki = 36.9 nM [5]
Drug Info IC50 = 0.88 nM [69]
Drug Info IC50 = 3530 nM [4]
Drug Info Ki = 3320 nM [15]
Drug Info Ki = 1.03 nM [6]
(+/-)-nantenine Drug Info Ki = 7265 nM [86]
(+/-)-TRANS-U-50488 METHANESULFONATE Drug Info IC50 = 1 nM
(-)-cyclorphan Drug Info IC50 = 1.7 nM [16]
(-)-eseroline Drug Info IC50 = 300 nM
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) Drug Info IC50 = 244 nM [23]
1,10-bis-(Dmt-Tic-amino)decane Drug Info IC50 = 5425 nM [15]
1,4-bis-(Dmt-Tic-amino)butane Drug Info Ki = 5.72 nM [15]
1,6-bis-(Dmt-Tic-amino)hexane Drug Info IC50 = 2715 nM [15]
1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane Drug Info Ki = 2.21 nM [15]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 24 nM [39]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 451 nM [39]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 2147 nM [39]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info Ki = 589 nM [38]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info Ki = 983 nM [38]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info Ki = 705 nM [38]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info Ki = 2988 nM [38]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info Ki = 3364 nM [38]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info Ki = 1057 nM [38]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info Ki = 936 nM [38]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info Ki = 3433 nM [38]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info Ki = 771 nM [38]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info Ki = 11050 nM [38]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info Ki = 11430 nM [38]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info Ki = 4554 nM [38]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info Ki = 11540 nM [38]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info Ki = 1734 nM [38]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info Ki = 10390 nM [38]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info Ki = 272 nM [38]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info Ki = 407 nM [38]
1-benzhydryl-4-cyclopropylpiperidin-4-ol Drug Info Ki = 18365 nM [38]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info Ki = 377 nM [39]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info Ki = 8899 nM [38]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info Ki = 13230 nM [38]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info Ki = 273 nM [38]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info Ki = 412 nM [39]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info Ki = 74 nM [38]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info Ki = 940 nM [38]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info Ki = 1649 nM [39]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info Ki = 233 nM [70]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info Ki = 3599 nM [38]
14-O-phenylpropylnaltrexone Drug Info Ki = 0.34 nM [68]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info Ki = 1.7 nM [84]
17-methyl-4'-methyldihydromorphinone Drug Info Ki = 0.34 nM [27]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info Ki = 0.34 nM [84]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Drug Info IC50 = 1.15 nM [78]
2-Benzylaminomethyl-3-hydroxymorphinan Drug Info Ki = 190 nM [84]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info Ki = 15 nM [84]
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone Drug Info Ki = 1.74 nM [15]
3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone Drug Info Ki = 2.83 nM [15]
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone Drug Info Ki = 3.76 nM [15]
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone Drug Info IC50 = 7025 nM [15]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info Ki = 230 nM [20]
3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol Drug Info Ki = 63 nM [7]
3-desoxy-3-carboxamidonaltrexone Drug Info IC50 = 270 nM [69]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info Ki = 0.29 nM [46]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [93]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info Ki = 2700 nM [80]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info Ki = 341 nM [39]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info Ki = 6265 nM [39]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info Ki = 144 nM [39]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info Ki = 37 nM [39]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info Ki = 29 nM [39]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info Ki = 2298 nM [39]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info Ki = 147 nM [39]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info Ki = 3728 nM [39]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info Ki = 1.77 nM [46]
6-(2-benzylisoindolin-5-yloxy)nicotinamide Drug Info Ki = 1008 nM [49]
6-(2-phenethylisoindolin-5-yloxy)nicotinamide Drug Info Ki = 658.8 nM [49]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 4.09 nM [46]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 0.17 nM [49]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info Ki = 7.44 nM [49]
6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide Drug Info Ki = 643.47 nM [46]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info Ki = 22.26 nM [46]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info Ki = 150 nM [101]
6-desoxonaltrexone Drug Info IC50 = 4.4 nM [69]
6beta-naltrexol HCl Drug Info Ki = 2.12 nM [72]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info IC50 = 721 nM [96]
8-carboxamidocyclazocine Drug Info Ki = 0.31 nM [60]
Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 Drug Info Ki = 340 nM [73]
Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 Drug Info Ki = 360 nM [73]
Ac-RYYRIK-K-(NH2)-YAFGYPS Drug Info IC50 = 0.15 nM [25]
Ac-RYYRIK-K-(NH2)-YRFB Drug Info IC50 = 2.76 nM [25]
Ac-YGGFL-NH2 Drug Info Ki = 37.3 nM [56]
AIKO-150 Drug Info Ki = 0.19 nM [67]
AKUAMMINE Drug Info IC50 = 3000 nM
AMINOFENTANYL Drug Info IC50 = 2080 nM [26]
Antanal 1 Drug Info Ki = 2.38 nM [65]
Antanal 2 Drug Info Ki = 1.52 nM [65]
Benzyl derivative of M6G Drug Info Ki = 0.5 nM [11]
Beta-funaltrexamine Drug Info IC50 = 2.2 nM [76]
BIPHALIN Drug Info Ki = 1.4 nM [91]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info Ki = 14 nM [16]
BREMAZOCINE Drug Info IC50 = 0.5 nM [98]
BUTORPHAN Drug Info Ki = 0.12 nM [1]
C6S Drug Info Ki = 38.7 nM [108]
CARBOXYFENTANYL Drug Info Ki = 5400 nM [48]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 5.3 nM [43]
Clocinnamox Drug Info Ki = 3 nM [68]
CODEINONE Drug Info Ki = 459 nM [44]
CTOP Drug Info IC50 = 2.8 nM [65]
CYPRODIME Drug Info Ki = 10600 nM [8]
C[L-Ala-D-pro-L-Phe-D-trp] Drug Info IC50 = 48 nM [73]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info Ki = 37 nM [73]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info Ki = 40 nM [73]
C[L-Phe-D-pro-L-Phe-D-trp] Drug Info IC50 = 21 nM [73]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info IC50 = 260 nM [73]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] Drug Info Ki = 43 nM [73]
C[L-Phe-D-pro-L-Tyr-D-trp] Drug Info Ki = 120 nM [73]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Drug Info Ki = 170 nM [73]
C[L-Tyr-D-pro-L-Phe-D-trp] Drug Info Ki = 670 nM [73]
D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 Drug Info IC50 = 1350 nM [99]
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) Drug Info IC50 = 3.5 nM [99]
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) Drug Info IC50 = 3.7 nM [99]
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 Drug Info IC50 = 350 nM [99]
DADLE Drug Info IC50 = 24 nM [42]
DAMGO Drug Info Ki = 0.87 nM
DC6S Drug Info Ki = 196 nM [108]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 2.84 nM [28]
DELTORPHIN Drug Info IC50 = 910 nM [62]
DELTORPHIN-II Drug Info Ki = 638 nM [92]
Deprotected cogener of M6G Drug Info Ki = 3.5 nM [11]
DERMORPHIN Drug Info IC50 = 0.538 nM [25]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 4.79 nM [28]
DIHYDROAKUAMMINE Drug Info IC50 = 6000 nM
Dimepheptanol Drug Info Ki = 230 nM [101]
DM3A6S Drug Info Ki = 13.7 nM [108]
DM3B6S Drug Info Ki = 61.8 nM [108]
DM6S Drug Info Ki = 1.5 nM [108]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 0.11 nM [41]
Dmt-Pro-Emp-Phe-NH2 Drug Info Ki = 0.21 nM [41]
Dmt-Pro-Imp-Phe-NH2 Drug Info Ki = 0.32 nM [41]
Dmt-Pro-Mmp-Phe-NH2 Drug Info Ki = 0.18 nM [41]
Dmt-Pro-Phe-D-1-Nal-NH2 Drug Info Ki = 1.24 nM [34]
Dmt-Pro-Phe-D-2-Nal-NH2 Drug Info Ki = 1.52 nM [34]
Dmt-Pro-Phe-Phe-NH2 Drug Info Ki = 0.26 nM [41]
Dmt-Pro-Tmp-Phe-NH2 Drug Info Ki = 0.18 nM [41]
Dmt-Pro-Trp-D-2-Nal-NH2 Drug Info Ki = 2.38 nM [34]
DPDPE Drug Info Ki = 2120 nM
Dynorphin(1-8) Drug Info Ki = 340 nM [100]
ELAEOCARPENINE Drug Info Ki = 18000 nM [88]
ENDOMORPHIN 2 Drug Info IC50 = 15 nM [95]
ENDOMORPHIN-1 Drug Info Ki = 10.7 nM [74]
FALCARINDIOL Drug Info Ki = 1125 nM [51]
FLUPERAMIDE Drug Info Ki = 0.11 nM [9]
H-2',6'-dimethyltyrosine-Tic-OH Drug Info Ki = 1360 nM [82]
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH Drug Info IC50 = 769 nM [82]
H-Aba-ala-Gly-Phe-leu-OH Drug Info Ki = 1200 nM [37]
H-Aba-ala-Gly-Phe-Met-OH Drug Info Ki = 100 nM [37]
H-Aba-Gly-Gly-Phe-Leu-OH Drug Info Ki = 1200 nM [37]
H-Aba-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 640 nM [37]
H-Apa-ala-Gly-Phe-leu-OH Drug Info Ki = 1400 nM [37]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info Ki = 9.8 nM [37]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info Ki = 9.8 nM [37]
H-Cdp-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 19 nM [37]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 18 nM [37]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info Ki = 28 nM [37]
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 173 nM [3]
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 1.2 nM [3]
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info IC50 = 1.39 nM [3]
H-Dmt-Aba-Gly-NH-CH2-Bid Drug Info IC50 = 231 nM [24]
H-Dmt-Aba-Gly-NH-CH2-Ph Drug Info IC50 = 51 nM [24]
H-Dmt-Aba-Gly-NH-Ph Drug Info IC50 = 95 nM [24]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 Drug Info IC50 = 0.509 nM [13]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH Drug Info IC50 = 63 nM [13]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 Drug Info Ki = 290 nM [33]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH Drug Info Ki = 580 nM [33]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 Drug Info Ki = 200 nM [33]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH Drug Info Ki = 55 nM [33]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 Drug Info Ki = 170 nM [33]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH Drug Info Ki = 280 nM [33]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 Drug Info Ki = 330 nM [33]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH Drug Info Ki = 1400 nM [33]
H-Dmt-Tic-Asp-N(Me)-Ph Drug Info Ki = 364.3 nM [63]
H-Dmt-Tic-Asp-NH-Bzl Drug Info Ki = 309.4 nM [63]
H-Dmt-Tic-Asp-NH-Ph Drug Info Ki = 10.8 nM [63]
H-Dmt-Tic-D-Asp-N(Me)-Ph Drug Info Ki = 45 nM [63]
H-Dmt-Tic-D-Asp-NH-Ph Drug Info Ki = 7.49 nM [63]
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) Drug Info IC50 = 100 nM [23]
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 Drug Info Ki = 380 nM [10]
H-Dmt-Tic-Glu-NH2 Drug Info Ki = 1360 nM [10]
H-Dmt-Tic-Gly-N(Me)-Ph Drug Info Ki = 1.75 nM [63]
H-Dmt-Tic-Gly-NH-Bzl Drug Info Ki = 0.16 nM [63]
H-Dmt-Tic-Gly-NH-CH2-Bid Drug Info IC50 = 26.9 nM [24]
H-Dmt-Tic-Gly-NH-Ph Drug Info Ki = 0.16 nM [63]
H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph Drug Info Ki = 5.5 nM [29]
H-Dmt-Tic-Lys(Ac)-NH-Ph Drug Info IC50 = 1248 nM [29]
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph Drug Info Ki = 4.41 nM [29]
H-Dmt-Tic-Lys(Z)-NH-Ph Drug Info IC50 = 438 nM [29]
H-Dmt-Tic-Lys-NH-CH2-Ph Drug Info Ki = 4.05 nM [29]
H-Dmt-Tic-Lys-NH-Ph Drug Info IC50 = 1254 nM [29]
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H Drug Info IC50 = 5900 nM [14]
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H Drug Info IC50 = 5550 nM [14]
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H Drug Info IC50 = 1600 nM [14]
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid Drug Info IC50 = 62.5 nM [29]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid Drug Info Ki = 16.1 nM [63]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) Drug Info Ki = 11.8 nM [63]
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) Drug Info Ki = 5.93 nM [63]
H-Dmt-Tic-NH-CH2-Boa Drug Info IC50 = 169.9 nM [52]
H-Dmt-Tic-NH-CH2-Bta Drug Info IC50 = 129.1 nM [52]
H-Dmt-Tic-NH-CH2-CH2-NH2 Drug Info IC50 = 285.6 nM [47]
H-Dmt-Tic-NH-CH2-Imid Drug Info IC50 = 113.3 nM [52]
H-Dmt-Tic-NH-CH2-ImidPh Drug Info IC50 = 153.5 nM [52]
H-Dmt-Tic-NH-CH2-Indl Drug Info IC50 = 208.9 nM [52]
H-Dmt-Tic-NH-CH2-Indn Drug Info IC50 = 28.41 nM [52]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid Drug Info IC50 = 53.9 nM [29]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid Drug Info IC50 = 375 nM [29]
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid Drug Info IC50 = 39.7 nM [29]
H-mCpa-ala-Gly-Phe-leu-OH Drug Info Ki = 560 nM [37]
H-mCpa-ser-Gly-Phe-Leu-Thr-OH Drug Info Ki = 1100 nM [37]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 59 nM [43]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 Drug Info Ki = 1.17 nM [36]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info Ki = 0.55 nM [36]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info Ki = 1.74 nM [36]
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 Drug Info Ki = 26.3 nM [19]
H-Tyr-c[D-Orn-Aic-Glu]-NH2 Drug Info Ki = 4.21 nM [19]
H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 Drug Info IC50 = 0.38 nM [104]
H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 Drug Info IC50 = 0.41 nM [104]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 Drug Info IC50 = 520 nM [55]
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac Drug Info IC50 = 62 nM [17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H Drug Info IC50 = 97 nM [32]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info IC50 = 240 nM [32]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info IC50 = 93 nM [32]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc Drug Info IC50 = 460 nM [17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info IC50 = 81 nM [17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info IC50 = 28 nM [17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info IC50 = 55 nM [17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info IC50 = 76 nM [32]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 Drug Info IC50 = 350 nM [55]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Drug Info IC50 = 13 nM [55]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 Drug Info IC50 = 52 nM [55]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Drug Info IC50 = 9 nM [55]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl Drug Info IC50 = 74 nM [55]
H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 Drug Info IC50 = 156 nM [104]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 12 nM [37]
H-Tyr-Pro-Ala-Phe-NH2 Drug Info Ki = 225.9 nM [56]
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 Drug Info IC50 = 389 nM [23]
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 Drug Info IC50 = 253 nM [23]
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H Drug Info IC50 = 25.1 nM [47]
H-Tyr-Tic-Cha-Phe-OH Drug Info Ki = 3600 nM [33]
HERKINORIN Drug Info Ki = 12 nM [58]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info Ki = 1.85 nM [81]
KETOCYCLAZOCINE Drug Info Ki = 3.3 nM [67]
KNT-5 Drug Info Ki = 24 nM [87]
KNT-62 Drug Info Ki = 0.205 nM [85]
KNT-63 Drug Info Ki = 0.212 nM [85]
Leucine-enkephalin Drug Info Ki = 380 nM [100]
LOFENTANIL Drug Info IC50 = 0.25 nM [102]
LY-25582 Drug Info Ki = 0.15 nM [49]
M3A6S Drug Info Ki = 0.8 nM [108]
M3B6S Drug Info Ki = 36.9 nM [108]
M3IBu6S Drug Info Ki = 19.8 nM [108]
M3P6S Drug Info Ki = 0.7 nM [108]
M3Pr6S Drug Info Ki = 0.6 nM [108]
M3S Drug Info Ki = 101 nM [108]
M6S Drug Info Ki = 0.9 nM [108]
MC-CAM Drug Info Ki = 4.78 nM [83]
MCL-139 Drug Info Ki = 0.16 nM [16]
MCL-144 Drug Info IC50 = 16 nM [77]
MCL-145 Drug Info Ki = 0.2 nM [16]
MCL-147 Drug Info Ki = 1.5 nM [40]
MCL-149 Drug Info Ki = 1.3 nM [40]
MCL-153 Drug Info Ki = 29 nM [89]
MCL-154 Drug Info Ki = 66 nM [89]
MCL-182 Drug Info Ki = 3.7 nM [40]
MCL-183 Drug Info Ki = 7.1 nM [40]
MCL-428 Drug Info IC50 = 22 nM [35]
MCL-429 Drug Info IC50 = 6.4 nM [35]
MCL-431 Drug Info Ki = 4.8 nM [35]
MCL-432 Drug Info Ki = 3.7 nM [35]
MCL-433 Drug Info Ki = 1.4 nM [35]
MCL-434 Drug Info Ki = 5.3 nM [35]
MCL-435 Drug Info Ki = 1.2 nM [35]
MCL-443 Drug Info IC50 = 260 nM [35]
MCL-444 Drug Info IC50 = 16 nM [35]
MCL-445 Drug Info Ki = 22 nM [40]
MCL-446 Drug Info Ki = 12 nM [40]
MCL-447 Drug Info IC50 = 1500 nM [40]
MCL-448 Drug Info IC50 = 380 nM [40]
MCL-449 Drug Info IC50 = 10 nM [35]
MCL-450 Drug Info IC50 = 97 nM [30]
MCL-451 Drug Info Ki = 1100 nM [30]
MCL-457 Drug Info Ki = 160 nM [40]
MCL-458 Drug Info Ki = 5.8 nM [40]
Met-enkephalin Drug Info Ki = 19 nM [37]
METAZOCINE Drug Info IC50 = 94 nM [103]
MM3A6S Drug Info Ki = 34.2 nM [108]
MM3B6S Drug Info Ki = 444 nM [108]
MORPHICEPTIN Drug Info Ki = 135 nM [95]
MORPHINONE Drug Info Ki = 146 nM [44]
MR-1029 Drug Info IC50 = 6.8 nM [18]
MR-1526 Drug Info IC50 = 84 nM [18]
MR-2034 Drug Info Ki = 0.19 nM [67]
MR-2266 Drug Info IC50 = 2.9 nM [18]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info Ki = 11 nM [84]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info Ki = 17 nM [84]
N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 Drug Info Ki = 1062 nM [31]
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 Drug Info IC50 = 845 nM [31]
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 Drug Info IC50 = 988 nM [31]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info Ki = 1.7 nM [84]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info Ki = 0.26 nM [84]
N-isobutylnoroxymorphone Drug Info Ki = 5.57 nM [64]
NalBzOH Drug Info Ki = 0.2 nM [108]
Nalfurafine hcl Drug Info Ki = 0.582 nM [85]
Naltrexone-6-alpha-ol Drug Info Ki = 0.21 nM [67]
NOCICEPTIN Drug Info Ki = 3030 nM [54]
NORBINALTORPHIMINE Drug Info Ki = 28.2 nM [94]
O-DESMETHYL TRAMADOL Drug Info Ki = 8.6 nM [67]
ORIPAVINE Drug Info Ki = 286 nM [44]
OXYMORPHINDOLE Drug Info Ki = 66 nM [59]
Oxymorphone semicarbazone hydrochloride Drug Info Ki = 14.5 nM [100]
PHENAZOCINE Drug Info Ki = 0.2 nM [67]
RTI-5989-31 Drug Info Ki = 3.1 nM [45]
SALVINORIN A Drug Info Ki = 4370 nM [58]
SB-0304 Drug Info IC50 = 3640 nM [57]
SB-213698 Drug Info Ki = 284.14 nM [71]
SL-3111 Drug Info IC50 = 17000 nM [2]
SN-11 Drug Info Ki = 0.77 nM [71]
SN-23 Drug Info Ki = 23.61 nM [71]
SN-28 Drug Info Ki = 10.8 nM [97]
SNF-9007 Drug Info IC50 = 220 nM [22]
SOMATOSTATIN Drug Info IC50 = 6 nM [99]
SPIROINDANYLOXYMORPHONE Drug Info Ki = 10.6 nM [75]
THEBAINE Drug Info Ki = 7400 nM [44]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info IC50 = 5.2 nM [43]
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 Drug Info IC50 = 30.6 nM [106]
Tyr-(R)-Aba-Gly-Phe-NH2 Drug Info Ki = 2.245 nM [50]
Tyr-(R)-spiro-Aba-Gly-Phe-NH2 Drug Info IC50 = 49.81 nM [50]
Tyr-(S)-Aba-Gly-Phe-NH2 Drug Info Ki = 0.373 nM [50]
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 Drug Info Ki = 8.732 nM [50]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 2300 nM [22]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 150 nM [22]
Tyr-D-Ala-Gly-NMePhe Drug Info IC50 = 1000 nM [76]
Tyr-D-Ala-Gly-Phe-Met-NH2 Drug Info Ki = 0.5 nM [91]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Drug Info IC50 = 61 nM [66]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info Ki = 20 nM [17]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 160 nM [22]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 470 nM [22]
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 Drug Info Ki = 578.9 nM [107]
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 Drug Info IC50 = 3180 nM [105]
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 Drug Info Ki = 0.29 nM [107]
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 Drug Info Ki = 1700 nM [107]
Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 Drug Info Ki = 4400 nM [107]
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 Drug Info IC50 = 3400 nM [105]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 1000 nM [22]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1200 nM [22]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 210 nM [22]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 48 nM [22]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 2700 nM [22]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 71 nM [22]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info IC50 = 420 nM [22]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 100 nM [22]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 2600 nM [22]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info IC50 = 4200 nM [22]
Tyr-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 6.19 nM [41]
Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 Drug Info IC50 = 2660 nM [106]
Tyr-Pro-D-Phe-D-Pro-NH2 Drug Info IC50 = 557 nM [106]
Tyr-Pro-D-Phe-Pro-NH2 Drug Info IC50 = 109 nM [106]
Tyr-Pro-D-Phg-Phe-NH2 Drug Info Ki = 1347 nM [21]
Tyr-Pro-Dmt-Phe-NH2 Drug Info Ki = 2.63 nM [41]
Tyr-Pro-Emp-Phe-NH2 Drug Info Ki = 0.46 nM [41]
Tyr-Pro-Hfe-Phe-NH2 Drug Info Ki = 28.4 nM [21]
Tyr-Pro-Hfe-Pro-NH2 Drug Info Ki = 586 nM [21]
Tyr-Pro-Imp-Phe-NH2 Drug Info Ki = 0.45 nM [41]
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 Drug Info IC50 = 20.7 nM [106]
Tyr-Pro-L-(NMe)Phe-Pro-NH2 Drug Info IC50 = 170 nM [106]
Tyr-Pro-L-Phe-D-Pro-NH2 Drug Info IC50 = 28.7 nM [106]
Tyr-Pro-L-Phe-Pro-NH2 Drug Info IC50 = 552 nM [106]
Tyr-Pro-Mmp-Phe-NH Drug Info Ki = 0.22 nM [41]
Tyr-Pro-Phe-Ala-Bn Drug Info Ki = 122 nM [79]
Tyr-Pro-Phe-D-2-Nal-NH2 Drug Info IC50 = 19.5 nM [53]
Tyr-Pro-Phe-D-Ala-Bn Drug Info Ki = 8.67 nM [79]
Tyr-Pro-Phe-D-Phg-NH2 Drug Info Ki = 216 nM [21]
Tyr-Pro-Phe-D-Val-Bn Drug Info Ki = 4.97 nM [79]
Tyr-Pro-Phe-Hfe-NH2 Drug Info Ki = 74.5 nM [21]
Tyr-Pro-Phe-Phe-N(CH3)2 Drug Info Ki = 272.7 nM [61]
Tyr-Pro-Phe-Phe-NHCH3 Drug Info Ki = 29.17 nM [61]
Tyr-Pro-Phe-Phe-NHNH2 Drug Info Ki = 9.35 nM [61]
Tyr-Pro-Phe-Phe-OC(CH3)3 Drug Info Ki = 50.35 nM [61]
Tyr-Pro-Phe-Phe-OCH2CH3 Drug Info Ki = 14.96 nM [61]
Tyr-Pro-Phe-Phe-OCH2OH Drug Info Ki = 6.34 nM [61]
Tyr-Pro-Phe-Phe-OCH3 Drug Info Ki = 9.07 nM [61]
Tyr-Pro-Phe-Phg-NH2 Drug Info Ki = 26.9 nM [21]
Tyr-Pro-Phg-Phe-NH2 Drug Info Ki = 268 nM [21]
Tyr-Pro-Phg-Pro-NH2 Drug Info Ki = 1042 nM [21]
Tyr-Pro-Tmp-Phe-NH Drug Info Ki = 0.44 nM [41]
Tyr-Pro-Trp-D-Ala-Bn Drug Info Ki = 4.56 nM [79]
Tyr-Pro-Trp-D-Val-Bn Drug Info Ki = 2.32 nM [79]
Tyr-Pro-Trp-Gly-Bn Drug Info Ki = 56.23 nM [79]
Tyr-Sar-Phe-D-2-Nal-NH2 Drug Info IC50 = 1560 nM [53]
UFP-502 Drug Info IC50 = 26.92 nM [92]
UFP-512 Drug Info IC50 = 1724 nM [92]
YAWF-NH2 Drug Info Ki = 3190 nM [56]
YGGWL-NH2 Drug Info IC50 = 49.2 nM [56]
YGWFL-NH2 Drug Info IC50 = 132.4 nM [56]
YPAA-NH2 Drug Info Ki = 705 nM [56]
YPWA-NH2 Drug Info Ki = 72.7 nM [56]
YRFB Drug Info IC50 = 1.18 nM [25]
ZYKLOPHIN Drug Info Ki = 5880 nM [81]
[3H]U69593 Drug Info Ki = 692 nM [108]
[D-Ala2]Met-enkephalinamide Drug Info IC50 = 17.4 nM [103]
[Dcp1]Dyn A(1-11)-NH2 Drug Info Ki = 44.9 nM [28]
[Leu5]enkephalin Drug Info Ki = 9.43 nM [90]
[Tyr-Pro-Phe-NH-CH2-]2 Drug Info IC50 = 218 nM [12]
[Tyr-Pro-Phe-NH-]2 Drug Info IC50 = 1135 nM [12]
[Tyr-Pro-Phe-Phe-NH-CH2-]2 Drug Info IC50 = 3544 nM [12]
[Tyr-Pro-Phe-Phe-NH-]2 Drug Info IC50 = 518 nM [12]
Action against Disease Model Buprenorphine Drug Info For MOR/CHO cell line Ki: 12.4 nM [109]
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