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96 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27876250 60 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
27318985 8 Metabolism study and biological evaluation of bosentan derivatives.EBI University of Perugia
26988801 55 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
26200936 39 Applications of Fluorine in Medicinal Chemistry.EBI Bristol-Myers Squibb Research and Development
9083490 37 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
22931505 69 Chemokine receptor antagonists.EBI National Heart and Lung Institute
22862294 118 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 Ltd
22750010 30 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
20684563 176 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 A/S
19916528 3 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
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15055997 42 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 Inc.
14998318 112 Selective optimization of side activities: another way for drug discovery.EBI Prestwick Chemical Inc.
12502366 82 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
11585442 20 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 Co., Ltd
10821712 18 Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.EBI NeoGenesis, Inc.
9857090 158 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
9216842 28 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 Company
8691426 114 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
8410970 106 Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.EBI Warner-Lambert Company
1324321 20 Design of a functional hexapeptide antagonist of endothelin.EBI Warner-Lambert Company
 49 Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentanEBI TBA
 28 Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelinEBI TBA
 21 Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptideEBI TBA
 20 Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activityEBI TBA
20932745 26 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
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
 10 A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruriEBI TBA
 47 Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonistsEBI TBA
 26 Search for surrogates: A study of endothelin receptor antagonist structure activity relationshipsEBI TBA
 24 γ-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugsEBI TBA
 47 2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonistsEBI TBA
 55 1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonistsEBI TBA
 61 Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonistsEBI TBA
 52 Thiophenesulfonamides as endothelin receptor antagonistsEBI TBA
 138 Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonistsEBI TBA
 57 1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonistsEBI TBA
 15 The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317EBI TBA
 24 Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptorsEBI TBA
 30 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
 24 Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)EBI TBA
 25 Structure-activity relationships in a series of monocyclic endothelin analoguesEBI TBA
 18 Endothelin receptor ligands. replacement net approach to SAR determination of potent hexapeptidesEBI TBA
 28 Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His16]EBI TBA
17055724 14 Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.EBI CovX Research LLC
15139756 221 Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.EBI Actelion Pharmaceuticals Ltd
15139753 55 Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.EBI University of Innsbruck
15006391 50 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
12852756 5 Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.EBI GlaxoSmithKline
12729650 2 Solid-phase synthesis of endothelin receptor antagonists.EBI BASF AG
12643919 50 Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12617929 114 The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.EBI Actelion Pharmaceuticals Ltd
12617928 68 Bis-sulfonamides as endothelin receptor antagonists.EBI Actelion Pharmaceuticals Ltd
12372497 40 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
12190306 14 Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
11985472 185 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 & Co., Ltd
11844662 34 Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
11755336 43 The design and synthesis of a novel series of indole derived selective ET(A) antagonists.EBI Pfizer Inc
11689084 47 Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.EBI Abbott Laboratories
11425549 30 Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.EBI Novartis Institute for BioMedical Research
11312921 16 Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.EBI Texas Biotechnology Corporation
10956219 26 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
10853654 18 Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.EBI Iowa State University
10479299 55 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
10479298 60 Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.EBI Abbott Laboratories
10447946 48 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 AG
10377221 44 Butenolide endothelin antagonists with improved aqueous solubility.EBI Warner-Lambert Company
9873522 8 Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.EBI Takarazuka Research Institute
9873521 52 Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.EBI Takarazuka Research Institute
9703472 112 Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).EBI Abbott Laboratories
9379441 100 Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.EBI Abbott Laboratories
9171878 69 Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.EBI ImmunoPharmaceutics Inc.
9171877 92 Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.EBI ImmunoPharmaceutics Inc.
9089328 170 Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.EBI Warner-Lambert Company
8676339 143 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.EBI Abbott Laboratories
8667356 50 Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.EBI BASF AG
8632421 32 Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.EBI Abbott Laboratories
26565745 165 Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI Janssen Pharmaceutica N.V.
8308857 19 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
8201588 14 1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.EBI SmithKline Beecham Pharmaceuticals Ltd
7731010 56 Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.EBI Warner-Lambert Company
7636842 155 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 Company
7473559 85 Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.EBI Tsukuba Research Institute
29631962 252 Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI Phenex Pharmaceuticals AG
28462837 48 Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ETEBI St. John's University
26833890 18 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
25951978 38 Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives.BDB University of Karachi
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig