Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and …

…, J Jiang, J Childress, BM Raaka, A Colson…

Index: Moore, Susanna; Jaeschke, Holger; Kleinau, Gunnar; Neumann, Susanne; Costanzi, Stefano; Jiang, Jian-Kang; Childress, John; Raaka, Bruce M.; Colson, Anny; Paschke, Ralf; Krause, Gerd; Thomas, Craig J.; Gershengorn, Marvin C. Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3888 - 3896

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Citation Number: 67

Abstract

The substituted thieno [2, 3-d] pyrimidine 3 (Org 41841), a partial agonist for the luteinizing hormone/choriogonadotropin receptor (LHCGR) and the closely related thyroid-stimulating hormone receptor (TSHR), was fundamentally altered, and the resulting analogues were analyzed for their potencies, efficacies, and specificities at LHCGR and TSHR. Chemical modification of the parent compound combined with prior mutagenesis of TSHR provided ...