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101 articles for thisTarget


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

PMID
Data
Article Title
Organization
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI
Jagiellonian University Medical College
Metabolism study and biological evaluation of bosentan derivatives.EBI
University of Perugia
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI
Jagiellonian University Medical College
Applications of Fluorine in Medicinal Chemistry.EBI
Bristol-Myers Squibb Research and Development
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.EBI
Zeneca Pharmaceuticals
Chemokine receptor antagonists.EBI
National Heart and Lung Institute
The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.EBI
Actelion Pharmaceuticals
Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.EBI
China Pharmaceutical University
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.EBI
H. Lundbeck
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.EBI
The University of Mississippi
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.EBI
Encysive Pharmaceuticals
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.EBI
Tanabe Seiyaku
Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.EBI
Neogenesis
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.EBI
Warner-Lambert
Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.EBI
Tsukuba Research Institute
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.EBI
Warner-Lambert
Design of a functional hexapeptide antagonist of endothelin.EBI
Warner-Lambert
 
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentanEBI
TBA
 
Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelinEBI
TBA
 
Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptideEBI
TBA
 
Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activityEBI
TBA
Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ET(A) antagonists.EBI
St. John'S University
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical and Public Health Institute
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI
Università
 
A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruriEBI
TBA
 
Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonistsEBI
TBA
 
Search for surrogates: A study of endothelin receptor antagonist structure activity relationshipsEBI
TBA
 
γ-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugsEBI
TBA
 
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonistsEBI
TBA
 
1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonistsEBI
TBA
 
Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonistsEBI
TBA
 
Thiophenesulfonamides as endothelin receptor antagonistsEBI
TBA
 
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonistsEBI
TBA
 
1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonistsEBI
TBA
 
The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317EBI
TBA
 
Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptorsEBI
TBA
 
Discovery of substituted 8,9-dicarboxyldibenzo [2,3:5,6] bicyclo [5.2.0] nonan-4-ones with moderate binding affinity to the endothelin ETA and ETB receptorsEBI
TBA
 
Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)EBI
TBA
 
Structure-activity relationships in a series of monocyclic endothelin analoguesEBI
TBA
 
Endothelin receptor ligands. replacement net approach to SAR determination of potent hexapeptidesEBI
TBA
 
Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His16]EBI
TBA
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.EBI
Covx Research
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.EBI
Actelion Pharmaceuticals
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.EBI
University of Innsbruck
Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.EBI
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.EBI
Glaxosmithkline
Solid-phase synthesis of endothelin receptor antagonists.EBI
Basf
Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.EBI
Actelion Pharmaceuticals
Bis-sulfonamides as endothelin receptor antagonists.EBI
Actelion Pharmaceuticals
Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.EBI
Tsukuba Research Institute
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and basEBI
Shionogi
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
The design and synthesis of a novel series of indole derived selective ET(A) antagonists.EBI
Pfizer
Pyridine alkaloids with activity in the central nervous system.EBI
University of Auckland
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.EBI
Abbott Laboratories
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.EBI
Novartis Institute For Biomedical Research
Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.EBI
Texas Biotechnology
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis.EBI
Centre Hospitalier Universitaire Vaudois (Chuv)
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.EBI
Iowa State University
From bosentan (TracleerŪ) to macitentan (OpsumitŪ): The medicinal chemistry perspective.EBI
Actelion Pharmaceuticals
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.EBI
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.EBI
Abbott Laboratories
Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.EBI
Basf
Butenolide endothelin antagonists with improved aqueous solubility.EBI
Warner-Lambert
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.EBI
Shanghaitech University
Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.EBI
Takarazuka Research Institute
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.EBI
Takarazuka Research Institute
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI
Rti International
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).EBI
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.EBI
Abbott Laboratories
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.EBI
Immunopharmaceutics
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.EBI
Immunopharmaceutics
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.EBI
Warner-Lambert
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.EBI
Abbott Laboratories
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.EBI
Basf
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.EBI
Abbott Laboratories
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI
Janssen Pharmaceutica
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.EBI
Smithkline Beecham Pharmaceuticals
Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.EBI
Warner-Lambert
Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.EBI
Warner-Lambert
Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.EBI
Tsukuba Research Institute
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI
Phenex Pharmaceuticals
Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ETEBI
St. John'S University
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
Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives.BDB
University of Karachi
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig