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AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.

AGN 194078 is a selective RARα agonist and binds to RARα with very high affinity, having a Kd value of 3 nM, while being unable to bind to RARβ and binding only very weakly (Kd=5600 nM) to RARγ. Furthermore, AGN 194078 maintains full transcriptional activity through RARα, with an EC50 value of 112 nM, but only activatedRARβ and RARγ with about 10% efficacy at the highest dose (1000 nM) tested[1].

[1]. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.

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