The first public molecular recognition database, BindingDB supports research, education and practice in drug discovery, pharmacology and related fields.

BindingDB contains 2.8M data for 1.2M Compounds and 9.2K Targets. Of those, 1,346K data for 622K Compounds and 4.5K Targets were curated by BindingDB curators. BindingDB is a FAIRsharing resource.

If BindingDB was of value to your research, please take a moment to donate to this nonprofit project. Your donation will let us provide you with more data and improved service.

Advanced Search

282 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.EBI
Abbott Laboratories
The discovery of quinoline based single-ligand human HEBI
Glaxosmithkline
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University Of Kansas
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.EBI
Bioprojet-Biotech
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.EBI
Icahn School Of Medicine At Mount Sinai
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.EBI
Novartis Institutes Of Biomedical Research (Nibr)
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI
University Of Regensburg
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.EBI
Astrazeneca
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI
University Of Minnesota
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI
The Alexander Shulgin Research Institute
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.EBI
Suven Life Sciences
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.EBI
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents.EBI
Jagiellonian University Medical College
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI
Janssen Research And Development
Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.EBI
Janssen Pharmaceutical Companies Of Johnson & Johnson
Biphenyl-ethyl-pyrrolidine derivatives as histamine h3 receptor modulators for the treatment of cognitive disorders.EBI
Temple University School Of Pharmacy
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.EBI
Teva Global R & D.
Novel 4-substituted-N,N-dimethyltetrahydronaphthalen-2-amines: synthesis, affinity, and in silico docking studies at serotonin 5-HT2-type and histamine H1 G protein-coupled receptors.EBI
University Of Florida
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.EBI
Universit£T Regensburg
Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.EBI
University Of Catania
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.EBI
Jagiellonian University Medical College
Benzylpiperidine variations on histamine H3 receptor ligands for improved drug-likeness.EBI
Johann Wolfgang Goethe University
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.EBI
Janssen Research And Development
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.EBI
United Arab Emirates University
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.EBI
Goethe University
Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold.EBI
Ku Leuven
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.EBI
Vrije Universiteit Amsterdam
Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain.EBI
Universit£
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.EBI
Vu University Amsterdam
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.EBI
Vu University Amsterdam
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.EBI
University Of Regensburg
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.EBI
Abbott Laboratories
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.EBI
University Of Regensburg
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.EBI
Johnson & Johnson Pharmaceutical Research & Development
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.EBI
Vu University Amsterdam
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.EBI
University Of Regensburg
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.EBI
Universit£
4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI
Abbott Laboratories
Novel azulene derivatives for the treatment of erectile dysfunction.EBI
Friedrich-Alexander University
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI
The University Of Sydney
Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: radiosynthesis and pharmacological evaluation.EBI
Eth Zurich (Swiss Federal Institute Of Technology)
Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).EBI
Pfizer
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.EBI
University Of Regensburg
Histamine H3 receptor as a drug discovery target.EBI
TBA
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI
Glaxosmithkline
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.EBI
TBA
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI
Cephalon
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists.EBI
Cephalon
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.EBI
Cephalon
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.EBI
The University Of Sydney
Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.EBI
Merck Research Laboratories
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI
Pfizer
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.EBI
National Institute Of Mental Health
Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies.EBI
Universidad De Navarra
Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.EBI
Cephalon
Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists.EBI
Cephalon
Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.EBI
Cephalon
Amine-constrained pyridazinone histamine H3 receptor antagonists.EBI
Cephalon
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.EBI
Cephalon
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI
National Institute Of Mental Health
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI
H. Lundbeck
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI
Meiji Seika Kaisha
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.EBI
Johnson & Johnson Pharmaceutical Research & Development
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.EBI
Argenta Discovery
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI
Hunter College And The Graduate Center Of The City University Of New York
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.EBI
F. Hoffmann-La Roche
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.EBI
Johann Wolfgang Goethe Universit£T
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.EBI
Jagiellonian University Medical College
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI
University Of Regensburg
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.EBI
F. Hoffmann-La Roche
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI
Purdue University
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.EBI
Johnson & Johnson Pharmaceutical Research And Development
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI
Abbott Laboratories
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.EBI
Abbott Laboratories
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.EBI
Novo Nordisk
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.EBI
Freie Universit£T Berlin
The first potent and selective non-imidazole human histamine H4 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.EBI
Freie Universit£T Berlin
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.EBI
Merck Research Laboratories
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.EBI
Cephalon
4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity.EBI
Cephalon
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.EBI
Cephalon
Synthesis of novel histamine H4 receptor antagonists.EBI
Pfizer
Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).EBI
Arena Pharmaceuticals
Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.EBI
Griffin Discoveries
Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI
Cephalon
4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists.EBI
Cephalon
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.EBI
Zhejiang University
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI
Cephalon
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.EBI
Vu University Amsterdam
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).EBI
Pfizer
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.EBI
Cephalon
Recent progress in synthesis and bioactivity studies of indolizines.EBI
University Of Botswana
Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists.EBI
Pfizer
Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity.EBI
Bioprojet-Biotech
Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.EBI
Bioprojet-Biotech
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.EBI
Jagiellonian University Medical College
Discovery of a series of potent arylthiadiazole H(3) antagonists.EBI
Merck Research Laboratories
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.EBI
Abbott Laboratories
Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.EBI
Universidad De Navarra
Indole- and benzothiophene-based histamine H3 antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Investigation of 4-piperidinols as novel H3 antagonists.EBI
Athersys
Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.EBI
F. Hoffmann-La Roche
Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.EBI
Johann Wolfgang Goethe University
Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.EBI
Johann Wolfgang Goethe University
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical And Public Health Institute
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI
Meiji Seika Kaisha
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI
Evotec (Uk)
In vitro studies on a class of quinoline containing histamine H3 antagonists.EBI
Abbott Laboratories
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI
Johnson & Johnson Pharmaceutical Research & Development
Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy.EBI
Hokkaido University
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI
Meiji Seika Kaisha
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.EBI
Merck Research Laboratories
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.EBI
Jagiellonian University Medical College
Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.EBI
Hokkaido University
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.EBI
Wyeth Research
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI
Tsukuba Research Institute
Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.EBI
Schering-Plough Research Institute
Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.EBI
Hoffmann-La Roche
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.EBI
Arena Pharmaceuticals
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI
Tsukuba Research Institute
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.EBI
Tsukuba Research Institute
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.EBI
Abbott Laboratories
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.EBI
Vanderbilt University
2-Aryloxymethylmorpholine histamine H(3) antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI
Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz
Fluorinated non-imidazole histamine H3 receptor antagonists.EBI
Johann Wolfgang Goethe-UniversitäT
Novel imidazole-based histamine H3 antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI
National Institute Of Mental Health
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.EBI
Jagiellonian University Medical College
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.EBI
National Institute Of Mental Health
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.EBI
The Schering Plough Research Institute
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
Novel H3 receptor antagonists with improved pharmacokinetic profiles.EBI
Arena Pharmaceuticals
Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.EBI
Kyowa Hakko Kogyo
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.EBI
Abbott Laboratories
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI
National Institute Of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
Glaxosmithkline
A new class of histamine H3 receptor antagonists derived from ligand based design.EBI
F. Hoffmann-La Roche
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.EBI
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors.EBI
Johnson & Johnson Pharmaceutical Research And Development
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.EBI
Abbott Laboratories
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.EBI
Johnson & Johnson Pharmaceutical Research And Development
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore.EBI
Johnson & Johnson Pharmaceutical Research And Development
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI
Hokkaido University
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.EBI
Novo Nordisk
Synthesis and SAR of novel histamine H3 receptor antagonists.EBI
Eli Lilly
Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor.EBI
Novo Nordisk
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI
Columbia University College Of Physicians And Surgeons
Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.EBI
Johann Wolfgang Goethe-UniversitäT
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI
Columbia University College Of Physicians And Surgeons
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.EBI
The Schering Plough Research Institute
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.EBI
Abbott Laboratories
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI
Novo Nordisk
Histamine HEBI
Heinrich Heine University D£Sseldorf
A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine HEBI
University Of Regensburg
Adenosine AEBI
Heinrich Heine University Duesseldorf
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.EBI
Freie UniversitäT Berlin
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.EBI
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.EBI
Abbott Laboratories
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.EBI
Huazhong University Of Science And Technology
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEBI
University Of Regensburg
Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease.EBI
Zhejiang University
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.EBI
Abbott Laboratories
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.EBI
Sungkyunkwan University
Non-imidazole heterocyclic histamine H3 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research And Development
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.EBI
Hokkaido University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable HEBI
Zhejiang University
Structural modifications in the distal, regulatory region of histamine HEBI
Jagiellonian University Medical College
Novel human histamine H(3) receptor antagonists.EBI
Johnson And Johnson Pharmaceutical Research And Development
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.EBI
The Schering Plough Research Institute
Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.EBI
Zhejiang University
New drug approvals for 2019: Synthesis and clinical applications.EBI
Zhengzhou University
Rational design of new multitarget histamine HEBI
Jagiellonian University Medical College
Isoquinolinone derivatives as potent CNS multi-receptor DEBI
Jiangsu Ocean University
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine HEBI
Jagiellonian University Medical College
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on HEBI
Universidade Federal De S£O Paulo
The Essential Medicinal Chemistry of Cannabidiol (CBD).EBI
University Of Minnesota
Novel pyrrolidinone derivative lacks claimed histamine HEBI
Heinrich Heine University D£Sseldorf
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.EBI
Freie UniversitäT Berlin
Pyridine alkaloids with activity in the central nervous system.EBI
University Of Auckland
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.EBI
Astrazeneca
In silico and in vitro studies on interaction of novel non-imidazole histamine HEBI
Jagiellonian University Medical College
Different antagonist binding properties of human and rat histamine H3 receptors.EBI
Freie UniversitäT Berlin
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge EBI
University Of Mississippi
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine HEBI
University Of Regensburg
Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands.EBI
Gedeon Richter
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.EBI
Chinese Academy Of Medical Sciences And Peking Union Medical College
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine HEBI
Jagiellonian University Medical College
Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands.EBI
Jagiellonian University Medical College
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.EBI
Palack£
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI
National Institute Of Neurological Disorders And Stroke
Discovery of novel steroidal histamine HEBI
Chemical Works Of Gedeon Richter
Rasagiline derivatives combined with histamine HEBI
Heinrich Heine University D£Sseldorf
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI
University Of Pennsylvania
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.EBI
Academy Of Scientific And Innovative Research (Acsir)
Optimization and preclinical evaluation of novel histamine HEBI
Jagiellonian University Medical College
New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine HEBI
Universit£
Search for new multi-target compounds against Alzheimer's disease among histamine HEBI
Jagiellonian University Medical College
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine HEBI
Suven Life Sciences
Design and in Vivo Characterization of AEBI
Medical College Of Wisconsin
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine HEBI
Vrije Universiteit Amsterdam
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).EBI
Csir-Central Drug Research Institute
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine HEBI
Heinrich Heine University D£Sseldorf
[EBI
University Of Regensburg
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.EBI
Julius Maximilian University Of W£Rzburg
4-tert-Pentylphenoxyalkyl derivatives - Histamine HEBI
Jagiellonian University Medical College
Design and synthesis of histamine HEBI
Hokkaido University
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.EBI
China Pharmaceutical University
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University Of Minnesota Twin Cities
Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.EBI
Astrazeneca
Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: high affinity and human/rat species-selective histamine H(3) receptor antagonists.EBI
Osaka University Of Pharmaceutical Sciences
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.EBI
Zhejiang University
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.EBI
United Arab Emirates University
Determination of the binding mode and interacting amino-acids for dibasic H3 receptor antagonists.EBI
Bioprojet-Biotech
Non-imidazole histamine HEBI
Medical University
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory
Histamine H4 receptor agonists.EBI
University Of Regensburg
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.EBI
Vrije Universiteit Amsterdam
Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold.EBI
Universit£
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.EBI
Vrije Universiteit Amsterdam
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.EBI
Vrije Universiteit
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.EBI
Osaka University
New lead elements for histamine HEBI
Pontificia Universidad Cat£Lica De Chile
Design, synthesis, and biological evaluation of novel oxadiazole- and thiazole-based histamine HEBI
Heinrich Heine University D£Sseldorf
Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine HEBI
Jagiellonian University Medical College
Novel indanone derivatives as MAO B/HEBI
Heinrich Heine University Duesseldorf
Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI
National Institute Of Diabetes And Digestive And Kidney Diseases
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.EBI
Novartis Institutes For Biomedical Research
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HEBI
Jagiellonian University Medical College
Identification of novel ?-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents.EBI
Csir-Central Drug Research Institute
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
University Of Texas At Austin
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.EBI
Iqog, Csic
Novel naphthyloxy derivatives - Potent histamine HEBI
Jagiellonian University Medical College
Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.EBI
Novartis Institutes For Biomedical Research
Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.EBI
Bioprojet-Biotech
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI
Northwestern University
Systematic Data Mining Reveals Synergistic H3R/MCHR1 Ligands.EBI
Freie Universit£T Berlin
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB
Yogi Vemana University
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.BDB
University Of Toronto
Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel.BDB
Novartis Institutes Of Biomedical Research Institute
Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity.BDB
Panjab University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University Of Leipzig
Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.BDB
UniversitÉ
Muscarinic cholinergic binding in rat brain.BDB
TBA
The characterization of [3H]sulpiride binding sites in rat striatal membranes.BDB
St, Marianna University School Of Medicine
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.BDB
Mgi Pharma