Compile Data Set for Download or QSAR
Report error Found 14225 Enz. Inhib. hit(s) with Target = 'Orexin/Hypocretin receptor type 1'
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50108620(CHEMBL3597953)
Affinity DataKi:  0.0600nMAssay Description:Binding affinity to OX1R (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2017
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50108620(CHEMBL3597953)
Affinity DataKi:  0.0600nMAssay Description:Antagonist activity at orexin-1 receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/14/2016
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50586152(CHEMBL5079059)
Affinity DataEC50:  0.0680nMAssay Description:Agonist activity at human OX1R expressed in CHO-K1 cells by FLIPR calcium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184008(US9150566, 45)
Affinity DataIC50: 0.100nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Rat)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50417257(SB-649868)
Affinity DataKi:  0.117nMAssay Description:Antagonist activity at recombinant rat OX1R expressed in CHO cells by FLIPR calcium based functional assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50419142(CHEMBL1830963)
Affinity DataKi:  0.126nMAssay Description:Antagonist activity at recombinant human OX1R expressed in CHO cells by FLIPR calcium based functional assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50439587(CHEMBL2418879)
Affinity DataEC50:  0.130nMAssay Description:Agonist activity at OX1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as calcium mobilization by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50419136(CHEMBL1830961)
Affinity DataKi:  0.158nMAssay Description:Antagonist activity at recombinant human OX1R expressed in CHO cells by FLIPR calcium based functional assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012606(CHEMBL3260826)
Affinity DataKi:  0.200nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50439587(CHEMBL2418879)
Affinity DataEC50:  0.220nMAssay Description:Agonist activity at human OX1 receptor overexpressed in CHO-RD-HGA16 cells assessed as calcium mobilization after 15 mins by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50417257(SB-649868)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to orexin receptor 1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012608(CHEMBL3260828)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50148575(CHEMBL3770503)
Affinity DataKi:  0.300nMAssay Description:Binding affinity to OX1R (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2017
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184006(US9150566, 43)
Affinity DataIC50: 0.300nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM183960(US9150566, Ref. 4)
Affinity DataIC50: 0.300nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012601(CHEMBL3260835)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012602(CHEMBL3260836)
Affinity DataKi:  0.300nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50417257(SB-649868)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity at recombinant human OX1R expressed in CHO cells by FLIPR calcium based functional assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50417257(SB-649868)
Affinity DataKi:  0.316nMAssay Description:Antagonist activity against human orexin 1 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2011
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318695(2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2...)
Affinity DataKi:  0.390nMAssay Description:Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318695(2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2...)
Affinity DataKi:  0.390nMAssay Description:Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701([(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,...)
Affinity DataKi:  0.398nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50314681((5-chloro-2-(2H-1,2,3-triazol-2-yl)phenyl)(6-(6-fl...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to OX1 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/18/2010
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50321509((5-chloro-2-(2H-1,2,3-triazol-2-yl)phenyl)((1R,5R)...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to OX1RMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012613(CHEMBL3260833)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184041(US9150566, 79)
Affinity DataIC50: 0.400nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50121795([Gly17]orexin-B | CHEMBL436915)
Affinity DataEC50:  0.410nMAssay Description:Agonist activity against human orexin 1 receptor; EC50; nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50060938(CHEMBL3394847)
Affinity DataKi:  0.410nMAssay Description:Antagonist activity at human OX1R by radioligand displacement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2016
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM604064(US11660293, Example 171 | US11660293, Example 173)
Affinity DataKi:  0.437nMAssay Description:CHO cells stably transfected with human Orexin type 1 receptors (CHO-hOX1) or HEK-293 cells transiently transfected with human Orexin type 2 receptor...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/2/2023
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50438824(CHEMBL2413365)
Affinity DataKi:  0.5nMAssay Description:Binding affinity to orexin receptor 1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012607(CHEMBL3260827)
Affinity DataKi:  0.5nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184009(US9150566, 46)
Affinity DataIC50: 0.5nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM183962(US9150566, Ref. 2)
Affinity DataIC50: 0.5nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM183973(US9150566, 10)
Affinity DataIC50: 0.5nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50012611(CHEMBL3260831)
Affinity DataKi:  0.5nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50121792([D-Ala19]orexin-B | CHEMBL439541)
Affinity DataEC50:  0.520nMAssay Description:Agonist activity against human orexin 1 receptor; EC50; nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701([(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,...)
Affinity DataKi:  0.550nMAssay Description:Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701([(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,...)
Affinity DataKi:  0.550nMAssay Description:Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50000984(CHEMBL3235265)
Affinity DataKi:  0.560nMAssay Description:Binding affinity to human OX1 receptor in cell membrane by in vitro radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2015
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM334712(US9732075, Example 4.70 | [(2S,3S)-2-(5-Chloro-4-m...)
Affinity DataIC50: 0.600nMAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2019
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701([(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,...)
Affinity DataKi:  0.600nMAssay Description:Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50321510((3-(7-fluoroquinazolin-2-yl)-3,9-di azabicyclo[4.2...)
Affinity DataKi:  0.600nMAssay Description:Binding affinity to OX1RMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701([(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,...)
Affinity DataKi:  0.600nMAssay Description:Binding affinity to orexin receptor 1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50321516(((1R,5R)-2-(7-fluoroquinazolin-2-yl)-2,6-diazabicy...)
Affinity DataKi:  0.600nMAssay Description:Binding affinity to OX1RMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/31/2012
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50121773([D-Asn20]orexin-B | CHEMBL386549)
Affinity DataEC50:  0.610nMAssay Description:Agonist activity against human orexin 1 receptor; EC50; nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM104692(US8569311, E-5)
Affinity DataKi:  0.631nMAssay Description:Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-typ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184022(US9150566, 60)
Affinity DataIC50: 0.700nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184065(US9150566, 103)
Affinity DataIC50: 0.700nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM184020(US9150566, 58)
Affinity DataIC50: 0.700nMT: 2°CAssay Description:Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2016
Entry Details
US Patent

TargetOrexin/Hypocretin receptor type 1(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM208487(US9266870, 3)
Affinity DataIC50: 0.700nMpH: 7.4 T: 2°CAssay Description:The antagonistic activities of the test compounds on human orexin-1 receptor (hOX1R) and orexin-2 receptor (hOX2R) were measured by modifying from th...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/17/2017
Entry Details
US Patent

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