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Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  0.890nMAssay Description:The binding affinities of disclosed compounds at the ketanserin binding site of the 5-HT2A receptor and the LSD binding site of the 5-HT2B receptor w...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2025
Entry Details
US Patent
PDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  0.890nMAssay Description:5-HT2A Receptor Radioligand Binding. Affinity of the test compounds for the 5-HT2A receptor was determined in radioligand binding experiments with [3...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2024
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetSerotonin 2 (5-HT2) receptor(Rat)
Virginia Commonwealth University

Curated by ChEMBL
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  2.5nMAssay Description:Compound was tested for binding affinity towards 5-hydroxytryptamine 2 receptor from frontal cortical regions of male Sprague-Dawley rat homogenates,...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  2.60nMAssay Description:Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human A549 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  2.70nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/17/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.10nMAssay Description:Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.16nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.20nMAssay Description:Binding affinity against 5-hydroxytryptamine 2A receptor human cloned receptors in HEK 293 cells using [3H]ketanserin as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.23nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.5nMAssay Description:Binding affinity towards 5-hydroxytryptamine 2A receptor using [125I]DOI as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.5nMAssay Description:Displacement of [125I]DOI from rat 5HT2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/22/2011
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.5nMAssay Description:Binding affinity to human 5HT2A receptor expressed in human A549 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  3.5nMAssay Description:In vitro binding to 5-hydroxytryptamine 2A receptor using [125 I]-DOIMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human A549 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  4.40nMAssay Description:Binding affinity was measured against 5-hydroxytryptamine 2A receptor by displacement of [3H]- ketanserin by lysergic acid amidesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  4.40nMAssay Description:Binding affinity of [3H]- ketanserin labelled towards Rat cortical 5-hydroxytryptamine 2A receptor using radioligand binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  5.20nMAssay Description:Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  5.20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/17/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  5.40nMAssay Description:Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  5.47nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSerotonin 2 (5-HT2) receptor(Rat)
Virginia Commonwealth University

Curated by ChEMBL
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  6.30nMAssay Description:Binding affinity against 5-hydroxytryptamine 2 receptor from rat frontal cortex using [125]-(R)-DOI as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  7.07nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  9.80nMAssay Description:Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  9.80nMAssay Description:Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM50241702([N-methyl-3H]LSD | CHEMBL463207 | lsd)
Affinity DataKi:  11.3nMAssay Description:Table S2 shows raw Ki data for the current study combined with data collected from the literature for the ten additional compounds.More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  12.0nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Rat)
University of Toronto

Curated by PDSP Ki Database
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataEC50:  15nMAssay Description:Functional potency at the rat 5-hydroxytryptamine 2A receptor as effective concentration EC50 for stimulating Phosphoinositide accumulationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM50241702([N-methyl-3H]LSD | CHEMBL463207 | lsd)
Affinity DataKd:  21.2nMAssay Description:Binding affinity to human 5HT2A receptor expressed in HEK293 cells by saturation binding methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 2A(Human)
Gilgamesh Pharmaceuticals

US Patent
LigandPNGBDBM21342((4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[...)
Affinity DataKi:  21.4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)