Page last updated: 2024-09-05

tbc-11251 and lu 135252

tbc-11251 has been researched along with lu 135252 in 5 studies

Compound Research Comparison

Studies
(tbc-11251)
Trials
(tbc-11251)
Recent Studies (post-2010)
(tbc-11251)
Studies
(lu 135252)
Trials
(lu 135252)
Recent Studies (post-2010) (lu 135252)
16732581961314

Protein Interaction Comparison

ProteinTaxonomytbc-11251 (IC50)lu 135252 (IC50)
Endothelin receptor type BHomo sapiens (human)0.016
Endothelin-1 receptorHomo sapiens (human)0.0008

Research

Studies (5)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (40.00)29.6817
2010's3 (60.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Berens, KL; Blok, N; Bourgoyne, AR; Brock, TA; Bui, H; Decker, ER; Dixon, RA; Holland, GW; Knowles, V; Wang, J; Wu, C; You, TJ1
Bolli, MH; Boss, C; Gatfield, J1
Lüscher, TF; Spieker, LE1
Brouwer, K; Gorczynski, R; Hartman, JC; Mandagere, A; Melvin, L1
Barton, M1

Reviews

3 review(s) available for tbc-11251 and lu 135252

ArticleYear
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
    Bioorganic & medicinal chemistry letters, 2016, 08-01, Volume: 26, Issue:15

    Topics: Bosentan; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Humans; Molecular Structure; Pyrimidines; Receptors, Endothelin; Structure-Activity Relationship; Sulfonamides

2016
Will endothelin receptor antagonists have a role in heart failure?
    The Medical clinics of North America, 2003, Volume: 87, Issue:2

    Topics: Animals; Bosentan; Cardiovascular Agents; Clinical Trials as Topic; Endothelin Receptor Antagonists; Endothelins; Heart Failure; Humans; Isoxazoles; Oligopeptides; Peptides, Cyclic; Phenylpropionates; Piperidines; Pyridines; Pyrimidines; Sulfonamides; Tetrazoles; Thiophenes; Treatment Outcome

2003
Endothelin antagonism and reversal of proteinuric renal disease in humans.
    Contributions to nephrology, 2011, Volume: 172

    Topics: Endothelins; Humans; Isoxazoles; Kidney Diseases; Phenylpropionates; Proteinuria; Pyridines; Pyrimidines; Receptor, Endothelin A; Thiophenes

2011

Trials

1 trial(s) available for tbc-11251 and lu 135252

ArticleYear
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.
    Journal of medicinal chemistry, 2004, Apr-08, Volume: 47, Issue:8

    Topics: Administration, Oral; Animals; Antihypertensive Agents; Biological Availability; Dose-Response Relationship, Drug; Double-Blind Method; Endothelin A Receptor Antagonists; Humans; Isoxazoles; Ligands; Male; Models, Molecular; Rats; Rats, Sprague-Dawley; Receptor, Endothelin A; Structure-Activity Relationship; Sulfones

2004

Other Studies

1 other study(ies) available for tbc-11251 and lu 135252

ArticleYear
Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes.
    Canadian journal of physiology and pharmacology, 2010, Volume: 88, Issue:6

    Topics: Adolescent; Adult; Aged; Antihypertensive Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Bosentan; Cell Culture Techniques; Cells, Cultured; Endothelin Receptor Antagonists; Enkephalin, D-Penicillamine (2,5)-; Estradiol; Female; Hepatocytes; Humans; Isoxazoles; Male; Middle Aged; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Organic Anion Transporters; Organic Anion Transporters, Sodium-Dependent; Phenylpropionates; Pyridazines; Pyrimidines; Sulfonamides; Symporters; Taurocholic Acid; Thiophenes; Young Adult

2010