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122 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27692854 100 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 Inc
27692832 7 Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.EBI Bioprojet-Biotech
27007611 115 Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI University of Regensburg
26718844 55 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
26360048 21 (2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.EBI Jagiellonian University Medical College
25993395 19 Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI Janssen Research and Development LLC
25827402 54 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.
25595684 62 Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.EBI Janssen Research and Development LLC
24697360 2 Biased ligand modulation of seven transmembrane receptors (7TMRs): functional implications for drug discovery.EBI Merck Research Laboratories
25455490 21 The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.EBI Janssen Research and Development LLC
24996140 26 Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.EBI Jagiellonian University Medical College
24735492 98 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
24495018 77 Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.EBI Janssen Research and Development LLC
24650714 21 Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.EBI United Arab Emirates University
24900647 8 Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.EBI Goethe University
23218604 30 Synthesis and evaluation of novel ligands for the histamine H4 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold.EBI KU Leuven
22003888 41 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
21944853 41 Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.EBI University of Regensburg
21782429 18 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
21348462 64 Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.EBI VU University Amsterdam
20409707 66 Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.EBI University of Regensburg
20171098 20 Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.EBI Abbott Laboratories
19791743 41 Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.EBI University of Regensburg
20192225 65 Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.EBI Griffin Discoveries BV
19524331 33 Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.EBI Johnson & Johnson Pharmaceutical Research & Development
19414267 49 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
19317445 53 N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.EBI University of Regensburg
19053770 68 Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.EBI Vrije Universiteit Amsterdam
18976927 83 Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity.EBI Universit£ degli Studi di Parma
15454206 1 Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.EBI Istanbul University
12657274 109 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott Laboratories
23099096 88 Novel azulene derivatives for the treatment of erectile dysfunction.EBI Friedrich-Alexander University
22216892 66 The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H2 receptor agonists.EBI University of Regensburg
21062081 47 Histamine H3 receptor as a drug discovery target.EBI TBA
22749391 72 Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.EBI Boehringer Ingelheim RCV GmbH & Co KG
22578490 35 Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI Cephalon Inc
22313227 78 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
21207959 69 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
20541426 46 Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI Meiji Seika Kaisha, Ltd
20299215 49 Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.EBI Argenta Discovery Ltd
19963380 38 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
18950149 75 Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI University of Regensburg
18459760 13 Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.EBI Gedeon Richter Plc
18077160 126 In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI Abbott Laboratories
12954048 36 The first potent and selective non-imidazole human histamine H4 receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development LLC
22189138 62 Synthesis of novel histamine H4 receptor antagonists.EBI Pfizer Inc
22153663 59 Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.EBI Griffin Discoveries BV
22153342 60 Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI Cephalon Inc
22019465 28 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
22014551 33 Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI Cephalon Inc
22007643 25 Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.EBI VU University Amsterdam
21955944 39 Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).EBI Pfizer Inc
21920751 39 Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.EBI Pfizer Inc
21920744 111 Tricyclic aminopyrimidine histamine H4 receptor antagonists.EBI Johnson & Johnson Pharmaceutical Research & Development
21498080 45 N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.EBI Jagiellonian University Medical College
21458260 71 Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.EBI Johnson & Johnson Pharmaceutical Research & Development
20690643 68 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI Meiji Seika Kaisha, Ltd
20667729 86 Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI Evotec (UK) Ltd
20452213 65 Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI Johnson & Johnson Pharmaceutical Research & Development
20384344 42 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, Ltd
19846299 52 Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.EBI Jagiellonian University Medical College
20045649 5 Synthesis and structural and pharmacological properties of cyclopropane-based conformationally restricted analogs of 4-methylhistamine as histamine H3/H4 receptor ligands.EBI Hokkaido University
19773175 41 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.EBI Johann Wolfgang Goethe University
19646882 72 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
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19520574 49 Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI Tsukuba Research Institute
19553110 16 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
18952421 60 Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18841880 82 Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18768318 37 Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
17571866 49 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
16942032 64 Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI Hokkaido University
16854056 8 Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.EBI Vrije Universiteit Amsterdam
16458504 37 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
16392798 46 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
16366610 41 Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development LLC
15634025 29 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI Novo Nordisk A/S
14741266 203 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
12723960 58 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
23891186 28 Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.EBI United Arab Emirates University
23668417 34 Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.EBI Boehringer Ingelheim RCV GmbH & Co KG
21075638 105 Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI Drug Discovery Laboratory AS
21044842 206 Histamine H4 receptor agonists.EBI University of Regensburg
18357976 53 Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.EBI Vrije Universiteit Amsterdam
17154494 11 Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.EBI Vrije Universiteit Amsterdam
15771452 49 N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.EBI Vrije Universiteit Amsterdam
14640553 104 Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.EBI Vrije Universiteit
12825954 68 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
29046238 17 1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI Universit£ degli Studi di Palermo
29723785 28 Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HEBI Jagiellonian University Medical College
27718472 77 Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.EBI Bioprojet-Biotech
28776992 110 Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI Northwestern University
28441580 23 The computer-aided discovery of novel family of the 5-HTEBI Jagiellonian University
26598975 16 A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.BDB University of Toronto
26640968 60 An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in -Cell Protection.BDB Broad Institute of Harvard and MIT
26685080 6 Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel.BDB Novartis Institutes of Biomedical Research Institute
7925364 13 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 Libre de Bruxelles
21040495 6 An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides.BDB Atatürk University
4151898 13 Muscarinic cholinergic binding in rat brain.BDB TBA
3828800 17 The characterization of [3H]sulpiride binding sites in rat striatal membranes.BDB St, Marianna University School of Medicine
19321349 46 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 Inc
18321037 129 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 Inc
16686531 26 Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.BDB MGI Pharma