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Nociceptin 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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NociceptinIC502.1 [1]
NociceptinKi0.18 [1]
CompBIC501.5 [1], 2.3 [2], 2.4 [3], 5.6 [4]
CompBKi0.4 [1], 2.3 [2]
Benzimidazole analogue, 7eIC500.72 [1], 2.1 [2]
N-Methyl-2-[2-oxo-3-[1-(4-propan-2-ylcyclohexyl)piperidin-4-yl]benzimidazol-1-yl]acetamideIC502.6 [1], 59.0 [2]
N-Methyl-2-[2-oxo-3-[1-(4-propan-2-ylcyclohexyl)piperidin-4-yl]benzimidazol-1-yl]acetamideKi0.7 [1], 1.7 [2], 31.0 [3]
(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-olKi77.0 [1], 77.4 [2], 212.0 [3]
(3R)-3-Methyl-4-[5-chloro-2-(tert-butylthio)-1H-benzoimidazole-6-yl]-1-piperazineethanolIC500.65 [1], 2.6 [2]
2-(4-(6-Chloro-2-(3-methylpentan-3-ylthio)-3H-benzo[d]imidazol-5-yl)piperazin-1-yl)ethanolIC500.66 [1], 1.2 [2]
2-(4-(6-Chloro-2-(pentan-3-ylthio)-3H-benzo[d]imidazol-5-yl)piperazin-1-yl)ethanolIC503.3 [1], 9.7 [2]
1-(1-(3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-oneIC5038.0 [1], 677.0 [2]
1-(1-(3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-oneKi4.0 [1], 47.0 [2]
2-(4-(2-(Tert-butylthio)-6-chloro-3H-benzo[d]imidazol-5-yl)piperazin-1-yl)ethanolIC5017.0 [1], 21.0 [2]
(1S,3R)-N-[[1-(3-Chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methylpyrazol-3-yl]methyl]-3-fluorocyclopentan-1-amineIC500.31 [1], 0.52 [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-olKi43.2 [1]
JTC-801 free baseIC5030.0 [1]
JTC-801 free baseKi8.2 [1]
Nociceptin(1-13)NH2IC500.35 [1]
Nociceptin(1-13)NH2Ki0.35 [1], 0.62 [2]
Ac-RYYRIK-NH2IC500.77 [1], 0.79 [2], 1.04 [3]
1-Benzyl-N-[3-(1'h,3h-Spiro[2-Benzofuran-1,4'-Piperidin]-1'-Yl)propyl]-D-ProlinamideIC500.15 [1], 0.27 [2]
1-Benzyl-N-[3-(1'h,3h-Spiro[2-Benzofuran-1,4'-Piperidin]-1'-Yl)propyl]-D-ProlinamideKi0.24 [1]
3-(1-Benzylpiperidin-4-yl)-1H-benzimidazol-2-oneIC50200.0 [1], 10000.0 [2]
1-Benzhydryl-4-phenylpiperidin-4-olKi13.0 [1]
1-(1-Benzylpiperidin-4-YL)-1,3-dihydro-indol-2-oneKi201.0 [1], 201.3 [2]
1-Phenyl-8-[(1S,2S)-2-phenylcyclohexyl]-1,3,8-triazaspiro[4.5]decan-4-oneIC506000.0 [1]
2-[3-[1-[3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]-2-oxobenzimidazol-1-yl]-N-methylacetamideIC5010.0 [1]
2-[3-[1-[3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]-2-oxobenzimidazol-1-yl]-N-methylacetamideKi1.0 [1]
1-(1-Cyclooctylpiperidin-4-yl)-3H-indol-2-oneKi1.39 [1], 1.4 [2]
1-[1-(4-Isopropyl-cyclohexyl)-piperidin-4-yl]-1,3-dihydro-indol-2-oneKi3.96 [1], 71.2 [2]
Benzimidazole analogue, 7hIC500.81 [1], 1.3 [2]
1-(2-Methoxyethyl)-3-[1-[3-(5-methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]benzimidazol-2-oneIC5060.0 [1]
1-(2-Methoxyethyl)-3-[1-[3-(5-methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]benzimidazol-2-oneKi4.0 [1], 4.07 [2]
trans-(+)-7-((4-o-Tolylpiperidin-1-yl)methyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olIC509.0 [1], 10000.0 [2]
trans-(+)-7-((4-o-Tolylpiperidin-1-yl)methyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olKi4.5 [1]
(2S)-6-Amino-2-[[(2S,3S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-(3-methylbutanoylamino)pentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]pentanoyl]amino]-3-methylpentanoyl]amino]hexanamideIC500.03 [1], 2.15 [2], 8.51 [3]
(5S,7R)-1-Methyl-7-[[4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-olIC5010.0 [1], 10000.0 [2]
(5S,7R)-1-Methyl-7-[[4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-olKi6.0 [1]
(1S,2S,6R,14R,15R,16R)-5-(Cyclopropylmethyl)-16-[(1S)-1-hydroxy-1-thiophen-2-ylethyl]-15-methoxy-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11-trien-11-olKi34.5 [1], 75.0 [2]
[6-Chloro-5-(4-ethylpiperazin-1-yl)-1H-benzimidazol-2-yl]-(4-hydroxy-1,4-dimethylcyclohexyl)methanoneIC501.3 [1], 1.4 [2], 27.0 [3]
(5S,7S)-7-[[4-(2,6-Dichlorophenyl)piperidin-1-yl]methyl]-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-olKi0.25 [1]
1-Phenyl-8-(acenaphthen-1-yl)-1,3,8-triazaspiro[4.5]decan-4-oneKi0.52 [1], 0.63 [2]
1-(1-Bicyclo[3.3.1]non-9-yl-piperidin-4-yl)-1,3-dihydro-indol-2-oneKi7.49 [1]
3-[5-(3,5-Difluorophenyl)-3-[[[(1S,3R)-3-fluorocyclopentyl]amino]methyl]-4-methylpyrazol-1-yl]propanenitrileIC504.6 [1], 8.2 [2]
1-(1-Cyclooctylmethyl-piperidin-4-yl)-1,3-dihydro-indol-2-oneKi6.0 [1], 6.04 [2]
8-[(1R,3Ar)-2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneIC504.4 [1]
8-[(1R,3Ar)-2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneKi0.39 [1]
1-[1-[1-(2-Chlorophenyl)ethyl]piperidine-4-yl]-1H-benzimidazole-2(3H)-oneIC505.9 [1], 10000.0 [2]
(6R,8S)-6-[[(3R,4R)-4-(2-Chloro-4-fluorophenyl)-3-hydroxypiperidin-1-yl]methyl]-5,6,7,8-tetrahydroquinolin-8-olIC5012.0 [1]
(6R,8S)-6-[[(3R,4R)-4-(2-Chloro-4-fluorophenyl)-3-hydroxypiperidin-1-yl]methyl]-5,6,7,8-tetrahydroquinolin-8-olKi11.0 [1]
1-(3,3-Diphenylpropyl)-4-[3-(trifluoromethyl)phenyl]piperidine-4-olKi116.0 [1]
8-(Diphenylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneKi23.0 [1]
(4R,7S,10S,13S,16R)-7-(4-Aminobutyl)-16-[[(2S,3R)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-phenylpropanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-10-[3-(diaminomethylideneamino)propyl]-13-methyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamideIC500.83 [1]
(4R,7S,10S,13S,16R)-7-(4-Aminobutyl)-16-[[(2S,3R)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-phenylpropanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-10-[3-(diaminomethylideneamino)propyl]-13-methyl-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamideKi0.83 [1]
8-[(2,6-Dichlorophenyl)methyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneKi2.3 [1]
8-(4,4-Dimethyl-2,3-dihydro-1H-naphthalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneKi1.3 [1]
N-[[(1S,5R)-8-[Bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-yl]methyl]acetamideKi20.0 [1]
N-[[5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]methyl]cyclopentanamineIC5028.0 [1]
1-(3,3-Diphenylpropyl)-4-[3-(trifluoromethyl)-4-chlorophenyl]piperidine-4-olKi225.0 [1]
4-[[4-[4-Chloro-3-(trifluoromethyl)phenyl]-4-hydroxypiperidin-1-yl]methyl]benzonitrileKi10000.0 [1]
4-(4-Chloro-3-trifluoromethyl-phenyl)-1-naphthalen-2-ylmethyl-piperidin-4-olKi879.0 [1]
4-[4-Chloro-3-(trifluoromethyl)phenyl]-1-[[4-(trifluoromethyl)phenyl]methyl]piperidin-4-olKi1194.0 [1]
1-Phenyl-8-[(1R,2S)-2-phenylcyclohexyl]-1,3,8-triazaspiro[4.5]decan-4-oneIC50300.0 [1], 310.0 [2]
(2S)-2-[(2-Fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)-N-propan-2-ylpropanamideKi0.23 [1]
(2S)-2-[(2-Fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)propanamideKi0.11 [1]
(2S)-2-[(2-Fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)-N-methyl-N-propan-2-ylpropanamideKi0.14 [1]
Unii-dqy244459TKi0.15 [1], 0.17 [2]
(2R)-2-[(2-Fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)-N-propan-2-ylpropanamideKi4.51 [1], 4.54 [2]
(2R)-2-[(2-Fluorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)propanamideKi5.61 [1]
N,N-Dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine;hydrochlorideKi0.1 [1], 0.3 [2]
8-[Bis(2-chlorophenyl)methyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-oneKi6.8 [1]
1-Phenyl-8-(1,2,3,4-tetrahydro-naphthalen-1-yl)-1,3,8-triaza-spiro[4.5]decan-4-oneKi1.4 [1], 2.1 [2]
8-Indan-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-oneKi0.7 [1], 1.2 [2]
3-[1-[3-(2,5-Dimethylphenoxy)-4-methylpentyl]piperidin-4-yl]-1H-benzimidazol-2-oneIC50131.0 [1]
3-[1-[3-(2,5-Dimethylphenoxy)-4-methylpentyl]piperidin-4-yl]-1H-benzimidazol-2-oneKi11.0 [1]
2-[4-[6-Chloro-2-(2-methylbutan-2-ylsulfanyl)-1H-benzimidazol-5-yl]piperazin-1-yl]ethanolIC502.5 [1], 5.6 [2]
1-[1-[3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]-3-(2-methylsulfanylethyl)benzimidazol-2-oneIC5042.0 [1]
1-[1-[3-(5-Methoxy-2-methylphenoxy)-4-methylpentyl]piperidin-4-yl]-3-(2-methylsulfanylethyl)benzimidazol-2-oneKi1.0 [1]
1-(1-Cyclooctylmethyl-piperidin-4-yl)-3-ethyl-1,3-dihydro-benzoimidazol-2-oneIC506.8 [1], 20.0 [2]
1-[1-(Cyclooctylmethyl)piperidine-4-yl]-1H-benzimidazole-2(3H)-oneIC506.8 [1], 20.0 [2]
(7R,9S)-7-[[(3S,4R)-3-Methyl-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olIC505.7 [1]
(7R,9S)-7-[[(3S,4R)-3-Methyl-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olKi3.5 [1]
(7R,9S)-7-[[(3R,4R)-4-(2-Chloro-4-fluorophenyl)-3-hydroxypiperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olIC505.0 [1]
(7R,9S)-7-[[(3R,4R)-4-(2-Chloro-4-fluorophenyl)-3-hydroxypiperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olKi4.4 [1]
(7R,9S)-7-[[(3S,4R)-3-(Hydroxymethyl)-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olIC507.3 [1]
(7R,9S)-7-[[(3S,4R)-3-(Hydroxymethyl)-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olKi4.3 [1]
(7R,9S)-7-[[(3S,4S)-3-Hydroxy-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olIC5018.0 [1]
(7R,9S)-7-[[(3S,4S)-3-Hydroxy-4-(2-methylphenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-olKi10.0 [1]
(2R)-1-Benzyl-N-(3-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropyl)pyrrolidine-2-carboxamideIC500.12 [1], 0.22 [2]
5-Chloro-3-(spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-8-olIC5021.3 [1]
5-Chloro-3-(spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-8-olKi2.2 [1]
(2S)-1-Benzyl-N-(3-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropyl)pyrrolidine-2-carboxamideIC5042.0 [1], 47.0 [2]
3-(Spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-8-olIC5053.9 [1]
3-(Spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-8-olKi2.4 [1]
3-(Spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-6-olIC50227.0 [1]
3-(Spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-6-olKi10.2 [1]
2-Phenoxy-N-(3-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropyl)benzamideIC504.0 [1], 8.2 [2]
2-Phenylmethoxy-N-(3-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpropyl)benzamideIC5083.0 [1], 110.0 [2]
1'-(1,2,3,4-Tetrahydroisoquinolin-3-ylmethyl)spiro[1,2-dihydroindene-3,4'-piperidine]IC50248.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Nociceptin receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/nociceptin-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). Quest Database™ Nociceptin receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/nociceptin-receptor-inhibitors-ic50-ki.
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