Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Article Details
- CitationCopy to clipboard
Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD, Wagner JR, Britt K, Lu KX, McMillen WT, Yingling JM
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
J Med Chem. 2006 Mar 23;49(6):2138-42.
- PubMed ID
- 16539403 [ View in PubMed]
- Abstract
Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus TGF-beta RII and MLK-7 kinases. Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 40 N/A N/A Details 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 81 N/A N/A Details 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 59 N/A N/A Details