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144 articles for thisTarget


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

PMID
Data
Article Title
Organization
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University of Kansas
N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.EBI
Bioprojet-Biotech
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI
University of Regensburg
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
(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.EBI
Jagiellonian University Medical College
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI
Janssen Research and Development
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.
Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.EBI
Janssen Research and Development
Biased ligand modulation of seven transmembrane receptors (7TMRs): functional implications for drug discovery.EBI
Merck Research Laboratories
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.EBI
Janssen Research and Development
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.EBI
Jagiellonian University Medical College
Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.EBI
Sanford-Burnham Medical Research Institute
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
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
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.EBI
University of Regensburg
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A.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
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.EBI
Griffin Discoveries
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
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.EBI
Vrije Universiteit Amsterdam
Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.EBI
Universit£
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
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
Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.EBI
Boehringer Ingelheim Rcv
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI
Cephalon
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
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
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI
Meiji Seika Kaisha
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
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI
University of Regensburg
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.EBI
Gedeon Richter
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI
Abbott Laboratories
The first potent and selective non-imidazole human histamine H4 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research and Development
Synthesis of novel histamine H4 receptor antagonists.EBI
Pfizer
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
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
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.EBI
Pfizer
Tricyclic aminopyrimidine histamine H4 receptor antagonists.EBI
Johnson & Johnson Pharmaceutical Research & Development
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.EBI
Jagiellonian University Medical College
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.EBI
Johnson & Johnson Pharmaceutical Research & Development
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)
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI
Johnson & Johnson Pharmaceutical Research & Development
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
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
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.EBI
Johann Wolfgang Goethe University
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI
Tsukuba Research Institute
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
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 a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI
Tsukuba Research Institute
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
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI
Hokkaido University
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.EBI
Vrije Universiteit Amsterdam
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine HEBI
University of Nottingham Biodiscovery Institute
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
Abolishing Dopamine DEBI
University of Regensburg
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
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI
Novo Nordisk
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
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
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEBI
University of Regensburg
Structure-Activity Relationship of Heterocyclic P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.EBI
Sungkyunkwan University
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 potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on HEBI
Universidade Federal De S£O Paulo
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
Alkyl derivatives of 1,3,5-triazine as histamine HEBI
Jagiellonian University Medical College
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine HEBI
Jagiellonian University Medical College
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI
National Institute of Neurological Disorders and Stroke
Rasagiline derivatives combined with histamine HEBI
Heinrich Heine University D£Sseldorf
New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine HEBI
Universit£
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.EBI
Shanghaitech University
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine HEBI
Vrije Universiteit Amsterdam
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine HEBI
Heinrich Heine University D£Sseldorf
[EBI
University of Regensburg
Design and synthesis of histamine HEBI
Hokkaido University
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University of Minnesota Twin Cities
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.EBI
United Arab Emirates University
Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.EBI
Boehringer Ingelheim Rcv
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory
Histamine H4 receptor agonists.EBI
University of Regensburg
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.EBI
Vrije Universiteit Amsterdam
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.EBI
Vrije Universiteit Amsterdam
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
1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI
Universit£
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HEBI
Jagiellonian University Medical College
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
The computer-aided discovery of novel family of the 5-HTEBI
Jagiellonian University
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.BDB
University of Toronto
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in -Cell Protection.BDB
Broad Institute of Harvard and Mit
Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel.BDB
Novartis Institutes of Biomedical Research Institute
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
An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides.BDB
AtatÜRk University
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
Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists.BDB
Astellas Pharma
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.BDB
Amgen
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.BDB
Mgi Pharma