 | Naltrexone | IC50 | 8.9 [1] |
| Naltrexone | Ki | 0.2 [1], 0.7 [2], 3.6 [3] |
 | Damgo | IC50 | 1.5 [1], 2.5 [2], 3.18 [3], 5.0 [4] |
| Damgo | Ki | 36.7 [1] |
 | Morphine | IC50 | 0.57 [1], 2.5 [2], 4.3 [3], 6.3 [4] |
| Morphine | Ki | 0.88 [1], 17.0 [2] |
 | Naloxone | IC50 | 7.3 [1] |
| Naloxone | Ki | 3.7 [1] |
 | Norbinaltorphimine | IC50 | 212.0 [1] |
| Norbinaltorphimine | Ki | 21.0 [1] |
 | Butorphan | IC50 | 20.0 [1] |
| Butorphan | Ki | 0.23 [1] |
 | Naltrindole | Ki | 6.3 [1] |
 | Cyclorphan | IC50 | 1.7 [1] |
| Cyclorphan | Ki | 0.06 [1] |
 | n-Methyl-2-phenyl-n-[(5r,7s,8s)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]dec-8-yl]acetamide | IC50 | 248.0 [1], 250.0 [2] |
 | Endomorphin-1 | IC50 | 3.2 [1], 14.0 [2] |
 | (1S,2S,6R,14R,15S,16R)-5-(Cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-ol | IC50 | 1.7 [1] |
 | 3-(3,4-Dimethyl-1-phenethyl-piperidin-4-yl)-phenol | IC50 | 1.1 [1], 2.0 [2] |
| 3-(3,4-Dimethyl-1-phenethyl-piperidin-4-yl)-phenol | Ki | 1.5 [1], 1.8 [2], 1.9 [3] |
 | Nalbuphine | IC50 | 1.0 [1], 110.0 [2], 752.0 [3] |
| Nalbuphine | Ki | 0.89 [1], 1.6 [2], 9.93 [3], 14.31 [4] |
 | Levorphanol | IC50 | 0.13 [1] |
| Levorphanol | Ki | 0.21 [1] |
 | Dermorphin | IC50 | 0.72 [1], 1.82 [2], 2.4 [3] |
| Dermorphin | Ki | 1.58 [1], 19.5 [2] |
 | Salvinorin A | Ki | 10000.0 [1] |
 | Clocinnamox | IC50 | 0.53 [1] |
| Clocinnamox | Ki | 0.25 [1], 2.98 [2], 3.0 [3] |
 | MC-Cam | IC50 | 0.97 [1] |
| MC-Cam | Ki | 0.46 [1], 4.78 [2], 4.8 [3] |
 | Bis[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] decanedioate | IC50 | 16.0 [1] |
| Bis[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] decanedioate | Ki | 0.09 [1] |
 | Dpdpe | IC50 | 610.0 [1] |
| Dpdpe | Ki | 504.0 [1], 10000.0 [2] |
 | Nociceptin | Ki | 270.0 [1], 437.0 [2], 1000.0 [3], 3030.0 [4] |
 | Diprenorphine | Ki | 0.07 [1], 0.12 [2], 0.2 [3], 0.27 [4], 0.33 [5] |
 | Endomorphin 2 | Ki | 0.69 [1], 1.33 [2], 3.2 [3], 5.3 [4], 8.23 [5] |
 | 4-(alpha-(4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide | IC50 | 320.0 [1], 4785.0 [2] |
| 4-(alpha-(4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide | Ki | 352.0 [1], 1300.0 [2] |
 | O-Desmethyltramadol | IC50 | 47.0 [1] |
| O-Desmethyltramadol | Ki | 8.6 [1], 11.0 [2], 13.0 [3] |
 | Bis[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] (E)-but-2-enedioate | IC50 | 610.0 [1] |
| Bis[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] (E)-but-2-enedioate | Ki | 0.2 [1] |
 | (1S,13R)-10-(Cyclopropylmethyl)-1,13-dimethyl-N-[2-(4-phenylphenyl)ethyl]-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-triene-4-carboxamide | IC50 | 150.0 [1] |
| (1S,13R)-10-(Cyclopropylmethyl)-1,13-dimethyl-N-[2-(4-phenylphenyl)ethyl]-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-triene-4-carboxamide | Ki | 0.3 [1] |
 | 3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenol | IC50 | 0.53 [1], 0.54 [2] |
| 3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenol | Ki | 0.62 [1] |
 | Leucine enkephalin | IC50 | 9500.0 [1] |
| Leucine enkephalin | Ki | 9.43 [1], 55.0 [2], 4800.0 [3] |
 | Ultram | IC50 | 7600.0 [1] |
| Ultram | Ki | 1600.0 [1], 2000.0 [2] |
 | Nalmefene | Ki | 0.24 [1], 0.44 [2], 0.91 [3] |
 | Alvimopan | IC50 | 1.7 [1], 3.16 [2] |
| Alvimopan | Ki | 0.32 [1], 0.47 [2] |
 | 3-[(3R,4R)-1-[(3S)-3-Cyclohexyl-3-hydroxypropyl]-3,4-dimethylpiperidin-4-yl]phenol | Ki | 0.04 [1], 0.1 [2], 0.15 [3] |
 | 8-Carboxamidocyclazocine | IC50 | 5.6 [1] |
| 8-Carboxamidocyclazocine | Ki | 0.31 [1] |
 | N-[(4R,4As,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]pyridine-4-carboxamide | IC50 | 2.29 [1], 19.5 [2] |
| N-[(4R,4As,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]pyridine-4-carboxamide | Ki | 0.37 [1] |
 | N-[(4R,4As,7S,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]isoquinoline-3-carboxamide | IC50 | 5.42 [1], 150.0 [2] |
| N-[(4R,4As,7S,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]isoquinoline-3-carboxamide | Ki | 0.55 [1] |
 | (1R,12R,13R)-20-(Cyclopropylmethyl)-7-thia-5,20-diazapentacyclo[10.5.3.01,13.02,10.04,8]icosa-2,4(8),5,9-tetraen-6-amine | Ki | 1.5 [1] |
 | (1R,12R,13R)-20-(Cyclobutylmethyl)-7-thia-5,20-diazapentacyclo[10.5.3.01,13.02,10.04,8]icosa-2,4(8),5,9-tetraen-6-amine | IC50 | 85.0 [1] |
| (1R,12R,13R)-20-(Cyclobutylmethyl)-7-thia-5,20-diazapentacyclo[10.5.3.01,13.02,10.04,8]icosa-2,4(8),5,9-tetraen-6-amine | Ki | 7.1 [1] |
 | N,N-Diethyl-4-[phenyl-[(1S,5R)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide | Ki | 72.0 [1], 72.3 [2], 317.0 [3] |
 | N,N-Dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine;hydrochloride | Ki | 0.26 [1], 0.6 [2], 310.0 [3] |
 | N-[(1S)-1-[4-[[2-[2-[7-[[2-[2-[[(4R,4As,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]heptylamino]-2-oxoethoxy]acetyl]amino]phenyl]-3-[3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]propyl]-4,4-difluorocyclohexane-1-carboxamide | IC50 | 40.0 [1] |
| N-[(1S)-1-[4-[[2-[2-[7-[[2-[2-[[(4R,4As,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]heptylamino]-2-oxoethoxy]acetyl]amino]phenyl]-3-[3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]propyl]-4,4-difluorocyclohexane-1-carboxamide | Ki | 51.8 [1] |
 | Fentanyl | IC50 | 1.3 [1] |
| Fentanyl | Ki | 2.9 [1], 3.97 [2] |
 | Codeine | IC50 | 105.0 [1] |
| Codeine | Ki | 727.0 [1], 6300.0 [2] |
 | Butorphanol | Ki | 0.12 [1], 0.22 [2] |
 | Levallorphan | Ki | 0.48 [1], 1.29 [2], 1.69 [3] |
 | Naloxonazine | Ki | 1.45 [1], 2.92 [2], 3.16 [3] |
 | 7-Benzylidenenaltrexone | Ki | 10.5 [1], 11.0 [2], 13.3 [3] |
 | CompB | IC50 | 2200.0 [1], 3400.0 [2] |
| CompB | Ki | 400.0 [1] |
 | Biphalin | IC50 | 1.4 [1] |
| Biphalin | Ki | 12.0 [1] |
 | JTC-801 free base | IC50 | 1507.0 [1] |
| JTC-801 free base | Ki | 102.0 [1], 102.9 [2] |
 | JDTic | Ki | 0.96 [1], 4.0 [2], 11.5 [3] |
 | Herkinorin | Ki | 12.0 [1] |
 | Leu-enkephalinamide | IC50 | 26.1 [1], 57.8 [2] |
| Leu-enkephalinamide | Ki | 11.4 [1] |
 | Salvinorin B | Ki | 10000.0 [1] |
 | 4-[[(4-Methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | IC50 | 24000.0 [1] |
| 4-[[(4-Methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Ki | 306.0 [1] |
 | 3-Desoxy-3-carboxamidonaltrexone | Ki | 0.71 [1] |
 | (4R,7S,10S,13R,16S,19R)-N-[(2S,3R)-1-Amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-10-[3-(diaminomethylideneamino)propyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-3,3-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | Ki | 1.06 [1], 2.33 [2], 2.96 [3] |
 | (1R,9R,10R)-17-(Cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amine | Ki | 3.7 [1] |
 | (1R,9R,10R)-17-(Cyclopropylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amine | Ki | 1.3 [1] |
 | (4As,9aR)-4a-ethyl-2-(2-phenylethyl)-1,3,4,9a-tetrahydro-[1]benzofuro[2,3-c]pyridin-6-ol | Ki | 0.7 [1], 0.9 [2] |
 | 1-Benzhydryl-4-phenylpiperidin-4-ol | Ki | 207.0 [1], 233.0 [2] |
 | (3R)-3-Methyl-4-[5-chloro-2-(tert-butylthio)-1H-benzoimidazole-6-yl]-1-piperazineethanol | IC50 | 97.0 [1], 1900.0 [2] |
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