93 articles for thisTarget
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Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.
H. Lundbeck
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
H. Lundbeck
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
H. Lundbeck
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
H. Lundbeck
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.
H. Lundbeck
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.
H. Lundbeck
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
H. Lundbeck
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
H. Lundbeck
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
H. Lundbeck
Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans.
H. Lundbeck
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
H. Lundbeck
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
H. Lundbeck
Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.
H. Lundbeck
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.
H. Lundbeck
Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
H. Lundbeck
The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors.
H. Lundbeck
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.
H. Lundbeck
Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole.
H. Lundbeck
Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors.
H. Lundbeck
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
H. Lundbeck
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
H. Lundbeck
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.
H. Lundbeck
The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.
H. Lundbeck
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists.
H. Lundbeck
Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles.
H. Lundbeck
Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.
H. Lundbeck
Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles.
H. Lundbeck
MACROCYCLIC PEPTIDOMIMETIC PROTEASE INHIBITOR AND USE THEREOF
Tencent Technology (Shenzhen)
BENZOTHIAZOLE AND QUINOLINE DERIVATIVES AND THEIR USE
Shanghai Yao Yuan Biotechnology Co.
Substituted 1′,2′-dihydro-3′H-spiro[cyclohexane-1,4′-pyrimido[5′,4′:4,5]pyrrolo[2,1-c][1,2,4]triazin]-3′-ones as cyclin-dependent kinase inhibitors
G1 Therapeutics
2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH
Bayer Aktiengellschaft
Substituted pyrrolo[2,1-f][1,2,4]triazines as kinase inhibitors
Daewoong Pharmaceutical
Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit MNK1 and MNK2
Effector Therapeutics
Substituted benzofuran, benzothiophene and indole Mcl-1 inhibitors
Vanderbilt University
Compounds as rearranged during transfection (RET) inhibitors
Glaxosmithkline Intellectual Property Development
Thiazolecarboxamides and pyridinecarboxamide compounds useful as PIM kinase inhibitors
Incyte Holdings
Inhibitors of PTP4A3 for the treatment of cancer
University of Virginia Patent Foundation
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.
Pfizer
2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
Merck Sharp & Dohme
Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions.
Aston University
Oxime-based compound, pharmaceutical composition containing the same and method for preparing the same
Chang Gung University
Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors.
Pontificia Universidad Catolica De Chile
Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions.
Universit�� Pierre Et Marie Curie
Substituted 2-azabicycles and their use as orexin receptor modulators
Janssen Pharmaceutica
Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as cFMS inhibitors
Array Biopharma
Functionalization of ß-Caryophyllene Generates Novel Polypharmacology in the Endocannabinoid System.
University of Bern
In vitro study of isoflavones and isoflavans as potent inhibitors of human 12- and 15-lipoxygenases.
Universidad De Santiago De Chile
Targeting GSK3 from Ustilago maydis: Type-II Kinase Inhibitors as Potential Antifungals.
Technische UniversitÄT Dortmund
Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Novartis Pharma
Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding.
TBA
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
Eli Lilly
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Smithkline Beecham Pharmaceuticals
Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile.
Hoechst Marion Roussel
[3H]SCH 23390 labels both dopamine-1 and 5-hydroxytryptamine1c receptors in the choroid plexus.
University of Pennsylvania
Characterization of the striatal M2 muscarinic receptor mediating inhibition of cyclic AMP using selective antagonists: a comparison with the brainstem M2 receptor.
Abbott Laboratories
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Glaxosmithkline