Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

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Alper PB, Marsilje TH, Mutnick D, Lu W, Chatterjee A, Roberts MJ, He Y, Karanewsky DS, Chow D, Lao J, Gerken A, Tuntland T, Liu B, Chang J, Gordon P, Seidel HM, Tian SS

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5255-8. doi: 10.1016/j.bmcl.2008.08.068. Epub 2008 Aug 22.

PubMed ID

18778936 [ View in PubMed

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Abstract

A novel series of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. Starting from a 3.4 microM high throughput screen hit, members of this series have been identified which are full agonists with functional potency <50 nM and oral bioavailability in mice.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Eltrombopag	Thrombopoietin receptor	EC 50 (nM)	38	N/A	N/A	Details