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77 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of novel BTK inhibitors with carboxylic acids.EBI
Merck & Co. Inc
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.EBI
GlaxoSmithKline
Challenges in the development of an MEBI
Vanderbilt University Medical Center
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 withEBI
Merck & Co.
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.EBI
Merck Research Laboratories
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.EBI
Merck & Co.
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.EBI
Merck & Co.
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.EBI
Actelion Pharmaceuticals Ltd
Discovery of Vibegron: A Potent and Selective▀3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI
Merck Research Laboratories
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI
Merck Research Laboratories
Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.EBI
Actelion Pharmaceuticals Ltd
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.EBI
AstraZeneca
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI
Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.EBI
Merck Research Laboratories
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.EBI
Jagiellonian University
Prediction of Thorough QT study results using action potential simulations based on ion channel screens.EBI
University of Oxford
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
GlaxoSmithKline
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.EBI
AstraZeneca
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.EBI
Merck & Co. Inc
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.EBI
AstraZeneca
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.EBI
Merck Research Laboratories
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.EBI
Merck Research Laboratories
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.EBI
Merck Research Laboratories
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.EBI
Merck Research Laboratories
Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.EBI
Squibb Institute for Medical Research
Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.EBI
TBA
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.EBI
Merck Frosst Centre for Therapeutic Research
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.EBI
Merck Research Laboratories
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.EBI
Merck Research Laboratories
Pyridyl amides as potent inhibitors of T-type calcium channels.EBI
Merck Research Laboratories
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.EBI
Wyeth Research
 
4-Biaryl-substituted dihydropyridines with an unusual antiperiplanar conformationEBI
TBA
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.EBI
Merck Research Laboratories
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI
Merck Research Laboratories
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.EBI
Merck Research Laboratories
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.EBI
Biogen
In Vitro and In Vivo Inhibition of the EBI
University of North Carolina at Chapel Hill
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of NaEBI
Merck & Co.
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.EBI
Merck & Co.
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.EBI
Merck & Co.
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3K? Immunomodulators.EBI
Merck & Co.
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.EBI
Novartis Institutes for BioMedical Research
Discovery of the First Orally Available, Selective KEBI
Praxis Precision Medicines
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).EBI
Sareum Ltd.
Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2.EBI
Redx Anti-Infectives Ltd
Optimization of Versatile Oxindoles as Selective PI3K? Inhibitors.EBI
Merck & Co.
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.EBI
University of Washington
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck & Co.
Discovery of AZD2716: A Novel Secreted Phospholipase AEBI
Astrazeneca
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.EBI
Merck Research Laboratories
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against EBI
GlaxoSmithKline
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.EBI
Recordati S.p.A.
Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.EBI
State University of New York
Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.EBI
AstraZeneca
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.EBI
TBA
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.EBI
The Walter and Eliza Hall Institute of Medical Research
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.EBI
Merck & Co.
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.EBI
Merck & Co., Inc.
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.EBI
Merck & Co.
Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.EBI
Università di Firenze
Successful reduction of off-target hERG toxicity by structural modification of a T-type calcium channel blocker.EBI
The Catholic University of Korea
Structure-activity relationships and discovery of a G protein biased ? opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.EBI
Trevena, Inc.
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.EBI
Merck & Co.
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.EBI
Merck & Co.
Design of Selective sPLAEBI
AstraZeneca
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.EBI
Idorsia Pharmaceuticals Ltd.
Discovery and evaluation of CaEBI
Idorsia Pharmaceuticals Ltd.
Discovery and evaluation of CaEBI
Idorsia Pharmaceuticals Ltd.
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.EBI
GlaxoSmithKline
Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.EBI
TBA
4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies.EBI
State University of New York
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid)EBI
Sage Therapeutics, Inc.
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.EBI
Merck & Co.
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
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.BDB
The Johns Hopkins University