 | Naltrexone | IC50 | 5.44 [1], 10.0 [2], 15.0 [3] |
| Naltrexone | Ki | 19.3 [1] |
 | Morphine | IC50 | 150.0 [1], 185.0 [2], 430.0 [3] |
| Morphine | Ki | 132.0 [1], 140.0 [2], 150.0 [3] |
 | Naltrindole | IC50 | 0.32 [1], 0.91 [2] |
| Naltrindole | Ki | 0.06 [1], 0.2 [2] |
 | Dpdpe | IC50 | 1.8 [1] |
| Dpdpe | Ki | 2.2 [1], 3.98 [2] |
 | Norbinaltorphimine | IC50 | 22.0 [1], 24.0 [2] |
| Norbinaltorphimine | Ki | 0.3 [1], 5.7 [2], 10.14 [3], 10.2 [4] |
 | Naloxone | IC50 | 62.0 [1] |
| Naloxone | Ki | 33.0 [1], 41.0 [2] |
 | Butorphan | Ki | 5.9 [1] |
 | n-Methyl-2-phenyl-n-[(5r,7s,8s)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]dec-8-yl]acetamide | IC50 | 4970.0 [1], 5000.0 [2], 5800.0 [3], 5844.0 [4] |
 | Damgo | Ki | 2000.0 [1] |
 | 4-(alpha-(4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide | IC50 | 1.3 [1], 2.0 [2], 2.2 [3] |
 | Cyclorphan | Ki | 1.9 [1] |
 | Levorphanol | IC50 | 2.9 [1], 5.1 [2] |
| Levorphanol | Ki | 4.2 [1] |
 | Biphalin | IC50 | 2.6 [1] |
 | (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 | 0.9 [1] |
 | Salvinorin A | Ki | 10000.0 [1] |
 | Fentanyl | IC50 | 187.0 [1], 187.4 [2], 431.0 [3] |
| Fentanyl | Ki | 570.0 [1], 679.0 [2], 1035.0 [3] |
 | Nociceptin | Ki | 2000.0 [1] |
 | N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu | IC50 | 83.0 [1] |
| N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu | Ki | 19.1 [1], 35.0 [2] |
 | Clocinnamox | IC50 | 0.19 [1] |
| Clocinnamox | Ki | 1.6 [1], 2.69 [2], 2.7 [3] |
 | 3-[(3R,4R)-1-[(3S)-3-Cyclohexyl-3-hydroxypropyl]-3,4-dimethylpiperidin-4-yl]phenol | Ki | 0.31 [1], 198.0 [2] |
 | Dynorphin A (1-11) amide | IC50 | 6.99 [1], 25.5 [2], 26.0 [3] |
| Dynorphin A (1-11) amide | Ki | 2.9 [1], 3.24 [2] |
 | MC-Cam | IC50 | 7.16 [1] |
| MC-Cam | Ki | 4.5 [1], 4.79 [2], 4.8 [3] |
 | Leucine enkephalin | Ki | 0.7 [1], 2.53 [2], 6.0 [3], 31.0 [4] |
 | Nalbuphine | IC50 | 353.0 [1] |
| Nalbuphine | Ki | 240.0 [1], 318.85 [2], 580.0 [3], 665.0 [4] |
 | Endomorphin-1 | Ki | 2765.0 [1], 5100.0 [2], 6080.0 [3] |
 | Oxymorphindole | Ki | 0.7 [1], 0.9 [2], 1.28 [3] |
 | 8-Carboxamidocyclazocine | Ki | 5.2 [1], 8.3 [2] |
 | 3-Desoxy-3-carboxamidonaltrexone | Ki | 110.0 [1], 550.0 [2] |
 | 3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenol | IC50 | 16.0 [1], 51.0 [2] |
| 3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenol | Ki | 30.0 [1], 31.0 [2] |
 | (D-Pen2,D-Pen5)-Enkephalin | IC50 | 1.3 [1] |
| (D-Pen2,D-Pen5)-Enkephalin | Ki | 2.4 [1], 3.2 [2], 3.3 [3] |
 | Oxymorphone | IC50 | 45.0 [1] |
| Oxymorphone | Ki | 50.0 [1], 70.0 [2], 145.0 [3] |
 | Dermorphin | IC50 | 197.0 [1], 210.0 [2], 295.0 [3] |
 | Nalmefene | Ki | 9.3 [1], 13.26 [2], 16.0 [3] |
 | Dynorphin A (1-13) | IC50 | 4.07 [1] |
| Dynorphin A (1-13) | Ki | 3.8 [1], 16.0 [2], 28.4 [3] |
 | 7-Benzylidenenaltrexone | Ki | 2.81 [1], 3.53 [2], 6.2 [3], 10.0 [4] |
 | 6beta-Naltrexol | IC50 | 23.0 [1], 32.0 [2] |
| 6beta-Naltrexol | Ki | 53.0 [1] |
 | 3-(3,4-Dimethyl-1-phenethyl-piperidin-4-yl)-phenol | Ki | 33.0 [1] |
 | (4R,7S,10R)-10-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-7-benzyl-3,3-dimethyl-6,9-dioxo-1,2-dithia-5,8-diazacycloundecane-4-carboxylic acid | Ki | 0.74 [1], 1.79 [2] |
 | 3-(4-Hydroxyphenyl)-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]propanamide | Ki | 450.0 [1], 5700.0 [2] |
 | (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 | 0.74 [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 | 29.0 [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 | 4.2 [1] |
 | (1R,9R,10R)-17-(Cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amine | Ki | 180.0 [1] |
 | (1R,9R,10R)-17-(Cyclopropylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amine | Ki | 150.0 [1] |
 | 4-[(4-Allyl-piperazin-1-yl)-phenyl-methyl]-N,N-diethyl-benzamide | IC50 | 5.0 [1], 8.0 [2], 15.9 [3] |
 | N,N-Diethyl-4-[phenyl-[(1S,5R)-8-(2-phenylethyl)-8-azabicyclo[3.2.1]octan-3-ylidene]methyl]benzamide | Ki | 0.24 [1], 42.1 [2] |
 | 4-(4-(3-Hydroxyphenyl)-1-(2-methylpentyl)piperidin-4-yl)-N,N-dimethylbenzamide | IC50 | 72.0 [1] |
| 4-(4-(3-Hydroxyphenyl)-1-(2-methylpentyl)piperidin-4-yl)-N,N-dimethylbenzamide | Ki | 11.0 [1] |
 | MET-enkephalin | IC50 | 6.4 [1] |
| MET-enkephalin | Ki | 1.1 [1], 2.0 [2] |
 | Butorphanol | Ki | 12.0 [1] |
 | beta-Funaltrexamine | Ki | 22.4 [1], 27.78 [2] |
 | Endomorphin 2 | Ki | 3385.0 [1], 6085.0 [2], 6420.0 [3] |
 | Deltorphin I | IC50 | 1.3 [1], 420.0 [2] |
| Deltorphin I | Ki | 1.73 [1] |
 | CompB | IC50 | 10000.0 [1] |
| CompB | Ki | 400.0 [1] |
 | JDTic | Ki | 29.6 [1], 36.11 [2], 188.0 [3] |
 | 2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]acetamide | IC50 | 600.0 [1] |
| 2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]acetamide | Ki | 24.0 [1] |
 | Herkinorin | Ki | 1170.0 [1] |
 | Salvinorin B | Ki | 10000.0 [1] |
 | Tyrosyl alanyl-glycyl-phenylalaninamide | IC50 | 724.44 [1] |
| Tyrosyl alanyl-glycyl-phenylalaninamide | Ki | 300.0 [1] |
 | 7-Spiroindanyloxymorphone | Ki | 1.4 [1], 2.75 [2], 3.3 [3] |
 | Enkephalin, pen(2,5)-4-chloro-phe(4)- | IC50 | 1.53 [1], 1.55 [2] |
| Enkephalin, pen(2,5)-4-chloro-phe(4)- | Ki | 0.3 [1] |
 | N-Methylnaltrindole | Ki | 0.02 [1], 0.49 [2] |
 | 4-[[(4-Methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | IC50 | 32000.0 [1] |
| 4-[[(4-Methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Ki | 1088.0 [1] |
 | Dynorphin A (swine) | IC50 | 2.54 [1] |
| Dynorphin A (swine) | Ki | 5.9 [1] |
 | (1S,9R,13R)-10-(Cyclopropylmethyl)-1,13-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol | Ki | 1.1 [1], 2.0 [2] |
 | 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 | 9.4 [1] |
 | CID 17379334 | Ki | 3.0 [1], 5.0 [2], 7.0 [3] |
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