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47 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].EBI
Roche Palo Alto
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.EBI
Roche Palo Alto
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.EBI
Roche Palo Alto
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.EBI
Roche Palo Alto
Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors.EBI
Roche Palo Alto
Discovery of a novel series of 4-quinolone JNK inhibitors.EBI
Roche Palo Alto
2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression.EBI
Roche Palo Alto
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.EBI
Roche Palo Alto
Discovery of potent and bioavailable GSK-3beta inhibitors.EBI
Roche Palo Alto
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.EBI
Roche Palo Alto
Design and synthesis of novel CCR3 antagonists.EBI
Roche Palo Alto
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.EBI
Roche Palo Alto
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitorsEBI
Roche Palo Alto
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.EBI
Roche Palo Alto
Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and pain.EBI
Roche Palo Alto
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.EBI
Roche Palo Alto
Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.EBI
Roche Palo Alto
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.EBI
Roche Palo Alto
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.EBI
Roche Palo Alto
Spiropiperidine CCR5 antagonists.EBI
Roche Palo Alto
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.EBI
Roche Palo Alto
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.EBI
Roche Palo Alto
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.EBI
Roche Palo Alto
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.EBI
Roche Palo Alto
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.EBI
Roche Palo Alto
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.EBI
Roche Palo Alto
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.EBI
Roche Palo Alto
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.EBI
Roche Palo Alto
Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.EBI
Roche Palo Alto
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.EBI
Roche Palo Alto
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.EBI
Roche Palo Alto
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.EBI
Roche Palo Alto
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents.EBI
Roche Palo Alto
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.EBI
Roche Palo Alto
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.EBI
Roche Palo Alto
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.EBI
Roche Palo Alto
Cyclic amide bioisosterism: strategic application to the design and synthesis of HCV NS5B polymerase inhibitors.EBI
Roche Palo Alto
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.EBI
Roche Palo Alto
Bifunctional compounds and use for reducing uric acid levelsBDB
Acquist
Heteroaromatic compounds and their use as dopamine D1 ligandsBDB
Pfizer
Cytotoxic and potent CYP1 inhibitors from the marine algae Cymopolia barbata.BDB
University of The West Indies
Beta adrenergic receptor binding in membrane preparations from mammalian brain.BDB
TBA
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.BDB
Istituto Di Biostrutture E Bioimmagini-Cnr