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SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.
Small molecule inhibitors have proven extremely useful for investigating signal transduction pathways and have the potential for development into therapeutics for inhibiting signal transductionExpand
Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542.
Transforming growth factor beta1 (TGF-beta1) is a potent fibrotic factor responsible for the synthesis of extracellular matrix. TGF-beta1 acts through the TGF-beta type I and type II receptors toExpand
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
Screening of our internal compound collection for inhibitors of the transforming growth factor beta1 (TGF-beta1) type I receptor (ALK5) identified several hits. Optimization of theExpand
Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type 1 Receptor (ALK5)
Screening of our internal compound collection for inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5) identified several hits. Optimization of the dihydropyrroloimidazoleExpand
The effects of SB 204070, a highly potent and selective 5‐HT4 receptor antagonist, on guinea‐pig distal colon
1 The pharmacology of a novel 5‐HT4 receptor antagonist, SB 204070 has been evaluated in the guinea‐pig isolated distal colon longitudinal muscle‐myenteric plexus (LMMP). 2 SB 204070 is a highlyExpand
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline
The evolution, synthesis, and biological activity of a novel series of 5-HT(2C) receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT(2C) affinityExpand
Serotonin 5‐HT3 and 5‐HT4 receptor antagonists
4-(6-Methoxy-2-naphthyl)butan-2-one and related analogues, a novel structural class of antiinflammatory compounds.
A series of compounds related to 4-(6-methoxy-2-naphthyl)butan-2-one has been prepared and tested for antiinflammatory activity by the cotton pellet granuloma method. Compounds possessing a smallExpand
Selective and functional 5‐hydroxytryptamine4 receptor antagonism by SB 207266
1 The pharmacology of a novel 5‐HT4 receptor antagonist, SB 207266 has been evaluated in vitro in the guinea‐pig distal colon longitudinal muscle myenteric plexus (LMMP) and in vivo in the dogExpand
Antagonism by SB 204070 of 5‐HT‐evoked Contractions in the Dog Stomach: an In‐vivo Model of 5‐HT4 Receptor Function
The ability of 5‐hydroxytryptamine (5‐HT) to evoke contractile activity in the gastric Heidenhain pouch was measured in conscious dogs using a method in which 5‐HT4 receptor‐antagonist activity canExpand
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