BDBM22567 3H]pyrilamine::CHEMBL511::Dorantamin::Mepyramine::N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine::N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine::PYRILAMINE::Pyranisamine::[3H]mepyramine::[3H]pyrilamine

SMILES CN(C)CCN(Cc1ccc(cc1)OC)c2ccccn2

InChI Key InChIKey=YECBIJXISLIIDS-UHFFFAOYSA-N

Data  25 KI  16 IC50  1 Kd  1 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 43 hits for monomerid = 22567   

TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKd:  0.851nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 3nMAssay Description:Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 34nMAssay Description:In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibitory concentration against IKr potassium channelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/1/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
University of Urbino

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.30nMAssay Description:Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 46.8nMAssay Description:Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Rat)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 5.75nMAssay Description:Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 0.820nMAssay Description:Binding affinity to human histamine H1 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 13nMAssay Description:Inhibitory activity against human Histamine H1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 0.0140nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2017
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 3.30nMAssay Description:Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.5nMAssay Description:Binding affinity to human histamine H1 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataEC50:  2.60nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 10nMAssay Description:Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of guinea pig histamine H1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.40nMAssay Description:Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2018
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.90nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/8/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  0.570nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/9/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  0.710nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/8/2019
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  0.740nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/9/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  0.950nMAssay Description:Binding affinity to human histamine H1 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.01nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/9/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.18nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/9/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.25nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/29/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.30nMAssay Description:Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2018
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.60nMAssay Description:Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.70nMAssay Description:Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/10/2015
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  1.70nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2016
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  2.09nMAssay Description:Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/21/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  2.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/25/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  3.70nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  3.98nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/29/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
In Depth
Date in BDB:
11/26/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  4.47nMAssay Description:Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Rat)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  4.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistamine H1 receptor(Human)
Adamed

Curated by ChEMBL
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  4.70nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/3/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi:  7.94E+3nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
Janssen Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/11/2012
Entry Details
PubMed
TargetHistamine H4 receptor(Human)
Vrije Universiteit Amsterdam

LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi: >1.00E+4nM ΔG°: >-7.09kcal/molepH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH4R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/28/2008
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22567(CHEMBL511 | PYRILAMINE | 3H]pyrilamine | N-[2-(dim...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/22/2011
Entry Details Article
PubMed