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Kappa opioid receptor Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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trans-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamideIC500.3 [1], 0.55 [2], 1.2 [3]
trans-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]-benzeneacetamideKi1.4 [1]
NorbinaltorphimineIC502.1 [1], 4.6 [2], 9.3 [3]
NorbinaltorphimineKi0.2 [1], 0.4 [2]
NaltrexoneIC501.86 [1], 200.0 [2]
NaltrexoneKi0.04 [1], 0.4 [2]
MorphineIC501705.1 [1]
MorphineKi24.0 [1], 260.0 [2]
Salvinorin AKi1.3 [1], 2.6 [2], 38.0 [3]
NaloxoneIC501.5 [1], 49.8 [2], 320.0 [3]
NaloxoneKi1.2 [1]
n-Methyl-2-phenyl-n-[(5r,7s,8s)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]dec-8-yl]acetamideIC502.0 [1], 8.0 [2]
ButorphanKi0.08 [1]
NaltrindoleKi10.1 [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-olIC501.2 [1]
CyclorphanKi0.03 [1]
LevorphanolIC504.0 [1]
LevorphanolKi2.3 [1]
DamgoKi2000.0 [1]
NociceptinKi2000.0 [1]
ClocinnamoxIC500.1 [1]
ClocinnamoxKi1.4 [1], 1.41 [2], 7.2 [3]
Salvinorin BKi155.0 [1]
4-[[(4-Methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamideIC50591.0 [1], 860.0 [2]
MC-CamIC509.81 [1]
MC-CamKi16.0 [1], 16.4 [2], 29.0 [3]
CID 44620907IC50570.0 [1], 660.0 [2], 750.0 [3]
DpdpeKi350.0 [1], 10000.0 [2]
NalbuphineIC5083.0 [1]
NalbuphineKi2.2 [1], 3.0 [2], 29.95 [3], 44.0 [4]
4-(alpha-(4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamideIC502480.0 [1]
4-(alpha-(4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamideKi3535.0 [1], 4169.0 [2]
3-(3,4-Dimethyl-1-phenethyl-piperidin-4-yl)-phenolKi17.0 [1], 52.0 [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-enedioateIC502400.0 [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-enedioateKi0.08 [1]
Bis[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] decanedioateKi0.05 [1]
3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenolIC501.2 [1], 3.2 [2]
3-((2R,3R,7S,9As)-2,3-dimethyl-7-phenyl-octahydro-1H-quinolizin-2-yl)phenolKi8.9 [1], 9.0 [2]
(1S,2S,6R,14R,15R,16R)-5-(Cyclopropylmethyl)-16-[(1S)-1-hydroxy-1-phenylethyl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-olKi0.04 [1], 0.49 [2]
DiprenorphineKi0.02 [1], 0.28 [2], 0.37 [3], 0.38 [4]
NalmefeneKi0.08 [1], 0.12 [2], 1.03 [3]
JDTicKi0.01 [1], 0.03 [2], 0.06 [3], 0.41 [4]
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]acetamideKi0.04 [1], 0.05 [2]
3-[(3R,4R)-1-[(3S)-3-Cyclohexyl-3-hydroxypropyl]-3,4-dimethylpiperidin-4-yl]phenolKi0.32 [1], 4.68 [2], 4.7 [3]
(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-carboxamideKi1.8 [1]
Divinorin propionateKi1.8 [1], 7.2 [2]
(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-amineKi0.05 [1]
(1S,2S,7S,8S,12R,20R,24R,32R)-11,33-Dimethyl-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17,27-tetrolKi7.7 [1], 21.7 [2], 1000.0 [3]
3-[[(1R,5S)-8-Benzyl-8-azabicyclo[3.2.1]octan-3-yl]oxy]benzamideIC50286.0 [1], 9680.0 [2]
3-[[(1R,5S)-8-Benzyl-8-azabicyclo[3.2.1]octan-3-yl]oxy]benzamideKi40.0 [1]
ButorphanolKi0.12 [1], 0.22 [2]
CompBIC501400.0 [1], 1600.0 [2]
CompBKi400.0 [1]
NalfurafineKi0.23 [1], 170.0 [2]
4-((R)-((2S,5R)-4-Allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamideIC5020.0 [1]
4-((R)-((2S,5R)-4-Allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamideKi130.0 [1], 3400.0 [2]
JTC-801 free baseIC507512.0 [1]
JTC-801 free baseKi1057.0 [1], 1057.5 [2]
Methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylateIC506.0 [1]
Methyl 4-[2-(3,4-dichlorophenyl)acetyl]-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylateKi0.45 [1], 360.0 [2]
14-MethoxymetoponKi15.1 [1], 25.2 [2], 304.0 [3]
HerkinorinKi90.0 [1]
Cyclazocine, (-)-Ki0.07 [1], 0.2 [2]
(S)-4-(4-((2-(3,5-Dimethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMideKi0.6 [1], 0.8 [2], 0.95 [3]
PF-4455242 free baseKi1.2 [1], 1.23 [2], 3.0 [3]
8-CarboxamidocyclazocineKi0.06 [1]
3-Desoxy-3-carboxamidonaltrexoneKi0.36 [1], 11.0 [2]
(3R)-N-[(2S)-1-[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideIC500.5 [1]
(3R)-N-[(2S)-1-[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideKi0.3 [1], 2.18 [2]
(1R,9R,10R)-17-(Cyclobutylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amineKi1.8 [1]
(1R,9R,10R)-17-(Cyclopropylmethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-amineKi0.18 [1]
1-Benzhydryl-4-phenylpiperidin-4-olKi364.0 [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-amineKi0.79 [1]
Methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-9-butanoyloxy-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylateKi4.0 [1], 4.9 [2]
(3R)-3-Methyl-4-[5-chloro-2-(tert-butylthio)-1H-benzoimidazole-6-yl]-1-piperazineethanolIC50120.0 [1], 180.0 [2]
Methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-9-acetyloxy-6a,10b-dimethyl-2-(3-methyl-1,2,4-oxadiazol-5-yl)-4,10-dioxo-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylateKi56.0 [1], 1000.0 [2]
2-(3,4-Dichlorophenyl)-1-[7-(pyrrolidin-1-ylmethyl)-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]ethanoneIC500.1 [1]
1-[1-(4-Isopropyl-cyclohexyl)-piperidin-4-yl]-1,3-dihydro-indol-2-oneKi148.0 [1], 148.7 [2], 369.0 [3]
(1S,2S,7S,8S,12R,20R,24R,32R)-11,33-Bis(cyclopropylmethyl)-27-methoxy-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17-triolKi0.39 [1], 17.0 [2], 28.0 [3]
1-[(1S,2S,7S,8S,12R,20R,24R,32R)-33-(Cyclopropylmethyl)-2,7,17,27-tetrahydroxy-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaen-11-yl]ethanoneKi23.6 [1], 104.0 [2]
(2S)-1-[2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]-N-[(2S)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S,3S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2R)-2-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamideIC50440.0 [1]
(2S)-1-[2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]-N-[(2S)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S,3S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2R)-2-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamideKi2.4 [1], 160.0 [2]
6-(4-(2-(Benzylamino)ethyl)phenoxy)nicotinamideKi18.41 [1], 136.26 [2]
6-(4-((Phenethylamino)methyl)phenoxy)nicotinamideKi1.15 [1], 8.38 [2]
Methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-9-acetyloxy-6a,10b-dimethyl-4,10-dioxo-2-(thiophene-2-carbonyl)-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylateKi36.0 [1], 38.0 [2]
Methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-9-(ethylcarbamoyloxy)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-2,4a,5,6,7,8,9,10a-octahydro-1H-benzo[f]isochromene-7-carboxylateKi462.0 [1], 10000.0 [2]
(1S,2S,7R,8S,12R,20R,24R,32R)-33-(Cyclopropylmethyl)-11-methyl-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,17,27-triolKi0.32 [1], 39.6 [2], 39.9 [3]
(1S,2S,7S,8S,12R,20R,24R,32R)-33-(Cyclopropylmethyl)-27-methoxy-11-methyl-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17-triolKi36.3 [1], 1000.0 [2]
N-[2-[Tert-butyl-[(4-chlorophenyl)methyl]amino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC501.6 [1], 84.0 [2], 107.0 [3]
N-[2-[(4-Chlorophenyl)methyl-propan-2-ylamino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC5010.0 [1], 392.0 [2], 400.0 [3]
N-[2-[(4-Bromophenyl)methyl-propan-2-ylamino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC5019.7 [1], 258.0 [2], 388.0 [3]
N-[2-[Benzyl(propan-2-yl)amino]ethyl]-2-(2,4,6-trimethylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC50113.0 [1], 930.0 [2], 1120.0 [3]
N-[2-[(4-Bromophenyl)methyl-propan-2-ylamino]ethyl]-2-(4-ethylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC5033.0 [1], 314.0 [2], 350.0 [3]
N-[2-[Tert-butyl-[(4-fluorophenyl)methyl]amino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC503.7 [1], 76.0 [2], 104.0 [3]
N-[2-[(4-Bromophenyl)methyl-tert-butylamino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC502.9 [1], 87.0 [2], 93.0 [3]
N-[2-[Tert-butyl-[(4-fluorophenyl)methyl]amino]ethyl]-2-(2,4,6-trimethylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC5085.0 [1], 880.0 [2], 1200.0 [3]
N-[2-[(4-Bromophenyl)methyl-tert-butylamino]ethyl]-2-(2,4,6-trimethylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC50106.0 [1], 710.0 [2], 1340.0 [3]
N-[2-[(4-Fluorophenyl)methyl-propan-2-ylamino]ethyl]-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-6-carboxamideIC5029.1 [1], 406.0 [2], 478.0 [3]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Kappa opioid receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/kappa-opioid-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 21). Quest Database™ Kappa opioid receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/kappa-opioid-receptor-inhibitors-ic50-ki.
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