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Orphagen Pharmaceuticals

San Diego, California, US

Orphagen is an industry leader in orphan nuclear receptor translational research and in screening of novel or unexplored receptors. We have 384-well screening capability and expertise in development and execution of innovative receptor assays. We also provide flexible nuclear receptor profiling and screening services on a contract basis.

Assets at Orphagen include a diverse small molecule screening library and broad expertise in screening at true orphan receptors where no ligands have previously been identified. Orphagen has pioneered discovery of ligands for a number of small molecule targets, including ROR-gamma, SF-1 and ROR-beta.

Assay quality is foremost among our objectives. For each receptor, assay Z-value and performance of standard agonist or antagonist are monitored to confirm assay quality. Relative efficacy and IC50 of test compounds are reported together with raw data in an Excel file. Secure... Show more »

Orphagen is an industry leader in orphan nuclear receptor translational research and in screening of novel or unexplored receptors. We have 384-well screening capability and expertise in development and execution of innovative receptor assays. We also provide flexible nuclear receptor profiling and screening services on a contract basis.

Assets at Orphagen include a diverse small molecule screening library and broad expertise in screening at true orphan receptors where no ligands have previously been identified. Orphagen has pioneered discovery of ligands for a number of small molecule targets, including ROR-gamma, SF-1 and ROR-beta.

Assay quality is foremost among our objectives. For each receptor, assay Z-value and performance of standard agonist or antagonist are monitored to confirm assay quality. Relative efficacy and IC50 of test compounds are reported together with raw data in an Excel file. Secure web-based data sharing is available upon request.

Selected Publications

  • Hirata K, Kotoku M, Seki N, Maeba T, Maeda K, Hirashima S, Sakai T, Obika S, Hori A, Hase Y, Yamaguchi T, Katsuda Y, Hata T, Miyagawa, Arita K, Nomura Y, Asahina K, Aratsu Y, Kamada M, Adachi T, Noguchi M, Doi S, Crowe P, Bradley E, Steensma R, Tao H, Fenn M, Babine R, Li X, Thacher S, Hashimoto H, Shiozaki M. 2016. SAR exploration guided by LE and Fsp3: Discovery of a selective and orally efficacious RORγ inhibitor. ACS Med Chem Lett. 7:23-7.
  • P.D. Crowe, McMinn J, Tao H, Steensma R, Auchus RJ, Thacher S. 2013. Steroidogenic Factor-1 Antagonist Suppression of Glucocorticoid Synthesis. Endocr Rev, 34(3):MON-LB-02.
  • Madoux, F., X. Li, P. Chase, G. Zastrow, M.D. Cameron, J.J. Conkright, P.R. Griffin, S. Thacher, and P. Hodder. Potent, selective and cell penetrant inhibitors of SF-1 by functional uHTS. Mol Pharmacol. (2008); 73: 1776-1784.
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Nuclear Receptor Assays
Price on request

Orphagen is an industry leader in orphan nuclear receptor translational research. We have developed and validated transcriptional and biochemical assays for a panel of nuclear receptors. We provide flexible nuclear receptor profiling and screening services.

Compounds can be screened against single or multiple receptors in... Show more »

Orphagen is an industry leader in orphan nuclear receptor translational research. We have developed and validated transcriptional and biochemical assays for a panel of nuclear receptors. We provide flexible nuclear receptor profiling and screening services.

Compounds can be screened against single or multiple receptors in single or multiple doses for selectivity profiling and/or IC50 determination. Library screening service is available upon request. We are experienced in drug discovery and we meet the highest industry standards .

We perform validated assays for the following receptors:

  • Metabolic receptors (FXR, LXRα,β; PPARα,δ,γ; and ERR α,β,γ)
  • The steroid hormone receptors (ER, AR, PR, VDR, and GR)
  • Retinoid receptors (RARα,β,γ and RXRα)
  • Orphan targets (RORα,β and LRH-1)
  • Custom receptor assay development upon request
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Receptor Deorphanization
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Orphagen has successfully identified ligands to nuclear receptors using its in house small molecule library. Custom screening strategies can be developed upon request. Orphagen's speciality is robust assay design for previously unexplored targets where validated ligands have not been identified.

Orphagen has successfully identified ligands to nuclear receptors using its in house small molecule library. Custom screening strategies can be developed upon request. Orphagen's speciality is robust assay design for previously unexplored targets where validated ligands have not been identified.

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High Throughput Screening
Small molecule Libraries
Biochemical Assays
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Biology
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Receptor Assays
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Biochemistry & Molecular Biology
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