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Orexin receptor 1 Inhibitors (IC50, Ki)

Structure
▲
▼
Compound Name
▲
▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
SuvorexantIC5050.0 [1], 199.0 [2]
SuvorexantKi0.55 [1], 0.6 [2]
[5-Methyl-2-(triazol-2-yl)phenyl]-(4-quinazolin-2-yl-1,4-diazepan-1-yl)methanoneIC5029.0 [1]
[5-Methyl-2-(triazol-2-yl)phenyl]-(4-quinazolin-2-yl-1,4-diazepan-1-yl)methanoneKi1.2 [1]
FilorexantIC5011.0 [1], 16.0 [2]
FilorexantKi2.2 [1], 2.5 [2], 2.9 [3]
[(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]methanoneKi1.8 [1]
AlmorexantIC5013.0 [1], 119.0 [2]
AlmorexantKi13.0 [1]
2-[(3R,6R)-6-Methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carbonitrileIC503200.0 [1], 3800.0 [2]
2-[(3R,6R)-6-Methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carbonitrileKi813.0 [1], 829.0 [2], 830.0 [3]
Urea, N-(2,4-dibromophenyl)-N'-((4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl)-Ki5.01 [1], 1644.0 [2], 3162.28 [3]
CID 25195495Ki0.3 [1], 0.32 [2], 0.76 [3]
2-[(3R,6R)-6-Methyl-1-(2-pyrimidin-2-ylbenzoyl)piperidin-3-yl]oxypyridine-4-carbonitrileIC504900.0 [1]
2-[(3R,6R)-6-Methyl-1-(2-pyrimidin-2-ylbenzoyl)piperidin-3-yl]oxypyridine-4-carbonitrileKi569.0 [1], 761.0 [2]
Methyl 2-[(3R,6R)-6-methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carboxylateIC501800.0 [1], 1809.0 [2]
Methyl 2-[(3R,6R)-6-methyl-1-[2-(triazol-2-yl)benzoyl]piperidin-3-yl]oxypyridine-4-carboxylateKi310.0 [1], 311.0 [2]
1-(2-Methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea;hydrochlorideIC5040.0 [1], 1000.0 [2]
1-(2-Methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea;hydrochlorideKi28.0 [1]
(2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamideIC5030.0 [1], 60.0 [2]
CID 10408514IC5010000.0 [1]
Mk-1064IC501789.0 [1]
Mk-1064Ki1584.0 [1]
CID 54765113IC506.0 [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-enamideKi8.14 [1]
[(2S)-2-[2-(4-Fluorophenoxy)ethyl]piperidin-1-yl]-(2-methyl-5-phenyl-1,3-thiazol-4-yl)methanoneIC5012.0 [1]
[(2S)-2-[2-(4-Fluorophenoxy)ethyl]piperidin-1-yl]-(2-methyl-5-phenyl-1,3-thiazol-4-yl)methanoneKi0.06 [1]
(3S,5S)-5-(2,6-Dimethoxyphenyl)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]methyl]pyrrolidin-2-oneIC50110.0 [1], 121.0 [2]
5-(2,6-Dimethoxyphenyl)-1-(4-(trifluoromethoxy)benzyl)pyrrolidin-2-oneIC50724.0 [1]
[(7R)-7-Methyl-4-(5,6,7,8-tetrahydroquinazolin-2-yl)-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5024.0 [1]
[(7R)-7-Methyl-4-(5,6,7,8-tetrahydroquinazolin-2-yl)-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi0.78 [1]
[(7R)-4-(6,7-Difluoroquinoxalin-2-yl)-7-methyl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5028.0 [1]
[(7R)-4-(6,7-Difluoroquinoxalin-2-yl)-7-methyl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi1.8 [1]
[(7R)-7-Methyl-4-quinazolin-2-yl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanoneIC5030.0 [1]
[(7R)-7-Methyl-4-quinazolin-2-yl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanoneKi0.39 [1]
[(7R)-7-Methyl-4-quinazolin-2-yl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneIC5026.0 [1]
[(7R)-7-Methyl-4-quinazolin-2-yl-1,4-diazepan-1-yl]-[2-(triazol-2-yl)phenyl]methanoneKi6.2 [1]
[(7R)-4-(1,3-Benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanoneIC5024.0 [1]
[(7R)-4-(1,3-Benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanoneKi4.1 [1]
(3R,5S)-1-(Dibenzofuran-2-ylmethyl)-5-(2-fluoro-6-methoxyphenyl)-3-hydroxypyrrolidin-2-oneIC50264.0 [1], 288.0 [2], 737.0 [3]
1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)ureaIC5040.0 [1]
1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)ureaKi18.0 [1]
LemborexantKi5.7 [1], 6.0 [2]
EmpaIC5010000.0 [1]
EmpaKi900.0 [1]
SeltorexantKi868.0 [1], 1277.0 [2]
MK-3697IC501986.0 [1]
MK-3697Ki3600.0 [1]
N-Benzyl-2-[1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]acetamideIC50119.0 [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)methanoneIC50630.0 [1]
(4-(6-Chlorobenzothiazole-2-yl)hexahydro-1H-1,4-diazepine-1-yl)(2,6-dimethoxyphenyl)methanoneKi216.0 [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]
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-acetamideIC5010000.0 [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)acetamideIC5019.0 [1]
N-Cyclopropyl-2-[6,7-dimethoxy-1-(naphthalen-2-ylmethyl)-3,4-dihydro-1H-isoquinolin-2-yl]-2-phenylacetamideIC5037.0 [1]
N-Benzyl-2-[1-[(3,4-dichlorophenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]acetamideIC50118.0 [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]methanoneKi5.5 [1], 15.0 [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)methanoneKi23.0 [1]
2-Benzylamino-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-butan-1-oneIC5010000.0 [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-enamideKi849.0 [1]
(S)-1-(2-(1H-Benzo[d]imidazol-2-ylthio)acetyl)-N-(2-(1H-pyrrol-1-yl)phenyl)pyrrolidine-2-carboxamideKi28.0 [1]
2-Anilino-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethylbutan-1-oneIC5010000.0 [1]
N-[1-Benzyl-2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl]-benzamideIC5010000.0 [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-diethylacetamideIC50119.0 [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-phenylacetamideIC5040.0 [1]
2-[(S)-2-(Benzoylamino)-3-phenylpropionyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5010000.0 [1]
2-(N-(3,4-Dimethoxyphenyl)sulfonyl-4-methylanilino)-N,N-diethylacetamideIC5010000.0 [1]
2-[(S)-2-(3-Thienylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC503670.0 [1]
2-[(S)-2-(2-Thienylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC501130.0 [1]
2-[(S)-2-(2-Thiazolylmethylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5010000.0 [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-fluorobenzamideIC505900.0 [1]
2-[(R)-2-(Benzylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC5010000.0 [1]
2-[(S)-2-(Benzylamino)-3,3-dimethylbutanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolineIC503850.0 [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-oneIC505500.0 [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-tetrahydroisoquinolineIC5010000.0 [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-tetrahydroisoquinolineIC5010000.0 [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 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 22 Feb. 2025, https://www.aatbio.com/data-sets/orexin-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 22). Quest Database™ Orexin receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/orexin-receptor-1-inhibitors-ic50-ki.
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