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Orexin receptor 2 Inhibitors (IC50, Ki)

Structure
▲
▼
Compound Name
▲
▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
SuvorexantIC500.4 [1], 56.0 [2], 138.0 [3]
SuvorexantKi0.35 [1], 0.4 [2], 11.8 [3]
[5-Methyl-2-(triazol-2-yl)phenyl]-(4-quinazolin-2-yl-1,4-diazepan-1-yl)methanoneIC5027.0 [1]
[5-Methyl-2-(triazol-2-yl)phenyl]-(4-quinazolin-2-yl-1,4-diazepan-1-yl)methanoneKi0.59 [1], 0.6 [2]
[(7R)-4-(6-Fluoroquinazolin-2-yl)-7-methyl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5027.0 [1]
[(7R)-4-(6-Fluoroquinazolin-2-yl)-7-methyl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi0.17 [1], 0.2 [2], 1.8 [3]
AlmorexantIC508.0 [1], 8100.0 [2]
AlmorexantKi4.7 [1], 8.0 [2]
FilorexantIC5011.0 [1], 17.0 [2]
FilorexantKi0.3 [1]
CID 25195495Ki0.4 [1], 1.29 [2], 8.5 [3]
2-[(3R,6R)-6-Methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carbonitrileIC509.0 [1], 13.0 [2]
2-[(3R,6R)-6-Methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carbonitrileKi1.6 [1]
Urea, N-(2,4-dibromophenyl)-N'-((4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl)-Ki5.01 [1], 6.0 [2], 3162.28 [3]
CID 54765113IC50417.0 [1]
CID 54765113Ki417.0 [1]
2-[(3R,6R)-6-Methyl-1-(2-pyrimidin-2-ylbenzoyl)piperidin-3-yl]oxypyridine-4-carbonitrileIC5028.0 [1]
2-[(3R,6R)-6-Methyl-1-(2-pyrimidin-2-ylbenzoyl)piperidin-3-yl]oxypyridine-4-carbonitrileKi1.3 [1]
Methyl 2-[(3R,6R)-6-methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carboxylateIC5022.0 [1]
Methyl 2-[(3R,6R)-6-methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carboxylateKi3.9 [1]
(2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamideIC505.0 [1], 11.0 [2]
CID 10408514IC5040.0 [1]
Mk-1064IC5018.0 [1]
Mk-1064Ki0.5 [1]
MK-3697IC5016.0 [1]
MK-3697Ki0.95 [1], 1.1 [2]
[(2S)-2-[2-(4-Fluorophenoxy)ethyl]piperidin-1-yl]-(2-methyl-5-phenyl-1,3-thiazol-4-yl)methanoneIC5014.0 [1]
[(2S)-2-[2-(4-Fluorophenoxy)ethyl]piperidin-1-yl]-(2-methyl-5-phenyl-1,3-thiazol-4-yl)methanoneKi1.0 [1]
(3S,5S)-5-(2,6-Dimethoxyphenyl)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]methyl]pyrrolidin-2-oneIC50126.0 [1], 128.0 [2]
5-(2,6-Dimethoxyphenyl)-1-(4-(trifluoromethoxy)benzyl)pyrrolidin-2-oneIC50158.0 [1]
[(3S)-4,4-Difluoro-3-quinolin-2-yloxypiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC504184.0 [1]
[(3S)-4,4-Difluoro-3-quinolin-2-yloxypiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi521.0 [1]
[(2R,5R)-5-Isoquinolin-1-yloxy-2-methylpiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5015.0 [1]
[(2R,5R)-5-Isoquinolin-1-yloxy-2-methylpiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi0.11 [1], 0.3 [2]
N-[(5,6-Dimethoxypyridin-2-yl)methyl]-5-(3-fluorophenyl)-2-(5-methylpyridin-3-yl)pyridine-4-carboxamideIC5016.0 [1]
N-[(5,6-Dimethoxypyridin-2-yl)methyl]-5-(3-fluorophenyl)-2-(5-methylpyridin-3-yl)pyridine-4-carboxamideKi0.9 [1], 0.91 [2]
N-[(5,6-Dimethoxypyridin-2-yl)methyl]-2-(5-methylpyridin-3-yl)-5-phenylpyridine-4-carboxamideIC5021.0 [1]
N-[(5,6-Dimethoxypyridin-2-yl)methyl]-2-(5-methylpyridin-3-yl)-5-phenylpyridine-4-carboxamideKi0.5 [1], 0.72 [2]
[(2R,5R)-5-(8-Fluoroquinolin-4-yl)oxy-2-methylpiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5018.0 [1]
[(2R,5R)-5-(8-Fluoroquinolin-4-yl)oxy-2-methylpiperidin-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi0.55 [1], 0.6 [2]
(3R,5S)-1-(Dibenzofuran-2-ylmethyl)-5-(2-fluoro-6-methoxyphenyl)-3-hydroxypyrrolidin-2-oneIC503.0 [1], 4.0 [2]
LemborexantKi0.44 [1], 3.0 [2]
EmpaKi1.1 [1]
SeltorexantKi9.0 [1]
N-Benzyl-2-[1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]acetamideIC508152.0 [1]
2-(3-Phenylpropionyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5010000.0 [1]
(4-(6-Chlorobenzothiazole-2-yl)hexahydro-1H-1,4-diazepine-1-yl)(2,6-dimethoxyphenyl)methanoneIC5098.0 [1]
(4-(6-Chlorobenzothiazole-2-yl)hexahydro-1H-1,4-diazepine-1-yl)(2,6-dimethoxyphenyl)methanoneKi25.0 [1]
1-(2-Bromophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi100.0 [1], 1995.26 [2]
1-(4-Bromo-2-chloro-phenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)-ureaKi6.31 [1], 5011.87 [2]
(E)-N-[(4R,4As,7R,7aR,12bS)-3-(benzenesulfonyl)-4a-hydroxy-9-methoxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamideIC5010000.0 [1]
(E)-N-[(4R,4As,7R,7aR,12bS)-3-(benzenesulfonyl)-4a-hydroxy-9-methoxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamideKi10000.0 [1]
1-(3-Bromophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi1000.0 [1], 10000.0 [2]
1-[(4S,5S)-2,2-Dimethyl-4-phenyl-1,3-dioxan-5-yl]-3-(2-propan-2-ylphenyl)ureaKi2511.89 [1], 10000.0 [2]
1-(2,5-Dichlorophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi63.1 [1], 5011.87 [2]
1-(2,6-Dichlorophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi5011.87 [1], 10000.0 [2]
1-(4-Bromophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi251.19 [1], 10000.0 [2]
N-[1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-2,2-dimethyl-propyl]-benzamideIC5010000.0 [1]
1-[(4S,5S)-2,2-Dimethyl-4-phenyl-1,3-dioxan-5-yl]-3-[2-(trifluoromethyl)phenyl]ureaKi100.0 [1], 10000.0 [2]
1-(2,4-Dimethylphenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi125.89 [1], 10000.0 [2]
1-[(4S,5S)-2,2-Dimethyl-4-phenyl-1,3-dioxan-5-yl]-3-(2-methoxyphenyl)ureaKi2511.89 [1], 10000.0 [2]
1-(2-Chlorophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi79.43 [1], 10000.0 [2]
1-[(4S,5S)-2,2-Dimethyl-4-phenyl-1,3-dioxan-5-yl]-3-(2-fluorophenyl)ureaKi398.11 [1], 10000.0 [2]
1-(4-Bromo-2-methylphenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi39.81 [1], 10000.0 [2]
1-(2-Chloro-5-methylphenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]ureaKi63.1 [1], 5011.87 [2]
2-[(4-Tert-Butyl-benzenesulfonyl)-p-tolyl-amino]-N,N-diethyl-acetamideIC505.0 [1]
1-(2,4-Dichloro-phenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)-ureaKi19.95 [1], 2511.89 [2]
2-[1-[(3,4-Dimethoxyphenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-(6-methoxy-2,3-dihydro-1H-inden-1-yl)acetamideIC50101.0 [1]
N-Cyclopropyl-2-[6,7-dimethoxy-1-(naphthalen-2-ylmethyl)-3,4-dihydro-1H-isoquinolin-2-yl]-2-phenylacetamideIC5080.0 [1]
N-Benzyl-2-[1-[(3,4-dichlorophenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]acetamideIC50281.0 [1]
1-((4S,5S)-2,2-Dimethyl-4-phenyl-[1,3]dioxan-5-yl)-3-(2-iodo-phenyl)-ureaKi79.43 [1], 5011.87 [2]
[3-[(4-Fluoro-3-methylphenoxy)methyl]piperidin-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanoneKi8.9 [1], 16.0 [2]
2-Amino-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-butan-1-oneIC5010000.0 [1]
[(3R)-3-[(4-Fluorophenoxy)methyl]piperidin-1-yl]-(2-methyl-5-phenyl-1,3-thiazol-4-yl)methanoneKi44.0 [1]
2-Benzylamino-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-butan-1-oneIC50910.0 [1]
(E)-N-[(4R,4As,7S,7aR,12bS)-3-(benzenesulfonyl)-4a-hydroxy-9-methoxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamideIC5010000.0 [1]
(E)-N-[(4R,4As,7S,7aR,12bS)-3-(benzenesulfonyl)-4a-hydroxy-9-methoxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamideKi10000.0 [1]
(S)-1-(2-(1H-Benzo[d]imidazol-2-ylthio)acetyl)-N-(2-(1H-pyrrol-1-yl)phenyl)pyrrolidine-2-carboxamideKi1.0 [1]
2-Anilino-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethylbutan-1-oneIC502100.0 [1]
N-[1-Benzyl-2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl]-benzamideIC50900.0 [1]
1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-2-(3-phenylpropylamino)butan-1-oneIC5010000.0 [1]
2-[2-Chloro-N-(3,4-dimethoxyphenyl)sulfonyl-5-(dimethylamino)anilino]-N,N-diethylacetamideIC505.0 [1]
(2R)-2-[(8S)-1-Chloro-3-ethyl-8-[2-[4-(trifluoromethyl)phenyl]ethyl]-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl]-N-methyl-2-phenylacetamideIC509.0 [1]
2-[(S)-2-(Benzoylamino)-3-phenylpropionyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC50195.0 [1]
2-(N-(3,4-Dimethoxyphenyl)sulfonyl-4-methylanilino)-N,N-diethylacetamideIC5019.0 [1]
2-[(S)-2-(3-Thienylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5035.0 [1]
2-[(S)-2-(2-Thienylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5025.0 [1]
2-[(S)-2-(2-Thiazolylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5059.0 [1]
1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-2-(2-phenylethylamino)butan-1-oneIC5010000.0 [1]
3-Bromo-N-[1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-fluorobenzamideIC5070.0 [1]
2-[(R)-2-(Benzylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC502900.0 [1]
2-[(S)-2-(Benzylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC50130.0 [1]
1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-2-dimethylamino-3-phenyl-propan-1-oneIC5010000.0 [1]
2-Benzyl-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethylbutan-1-oneIC5056.0 [1]
2-(Cyclohexylmethylamino)-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethylbutan-1-oneIC5010000.0 [1]
2-[(S)-2-(3-Pyridinylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC50240.0 [1]
2-[(S)-2-(Benzylamino)-3-phenylpropionyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5010000.0 [1]
2-[(S)-2-(2-Pyridinylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC501400.0 [1]
2-[(S)-2-(3,5-Dichlorobenzoylamino)-3-phenylpropionyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5030.0 [1]
2-[(4-Bromophenyl)methyl]-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethylbutan-1-oneIC502000.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Orexin receptor 2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/orexin-receptor-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Orexin receptor 2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/orexin-receptor-2-inhibitors-ic50-ki.
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