RECEPTOR BINDING AND PREDICTIVE TOXICOLOGY SERVICES

受体结合和预测毒理学服务

• 批准号: 10044353
• 负责人: JEFFREY BRYAN
• 金额: $ 44.65万
• 依托单位国家: 美国
• 财政年份: 2019
• 资助国家: 美国
• 起止时间: 2019-03-22 至 2020-03-21
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10044353
• 关键词: Affinity; Agonist; Area; Binding; Biological; Biological Assay; Catalogs; Chemical Structure; Contractor; Contracts; Development; Dopamine Receptor; Drug Kinetics; Drug abuse; Enzymes; Individual; Lead; Libraries; Ligands; Medical; Methods; National Institute of Drug Abuse; Pharmaceutical Preparations; Pharmacology; Process; Reporting; Safety; Services; Site; Source; Specific qualifier value; Specificity; Testing; Therapeutic; Toxic effect; Toxicology; drug development; in vitro Assay; novel; receptor; receptor binding; screening

1. This contract provides the NIDA Division of Therapeutics and Medical Consequences with reports in which the Contractor assesses the pharmacological specificity and potential toxicity of lead compounds by screening at a large number of biological targets. 2. This contract will also support studies to determine the affinity (IC50, Ki) and/or function (EC50, IC50) of test compounds for receptors at specified biological targets indicated by compound profiling or other sources. 3. This contract will provide a way to screen additional compounds, possibly large compound libraries, at one or more receptors or transporters in order to determine biological activity, with the objective of discovering specific receptor or transporter ligands with novel chemical structures. 4. This contract will provide assays to assess predictive toxicology in key areas that could indicate a candidate compound would have difficulties in the drug development process. 5. This contract will allow development of in vitro assays at targets that may be of importance in the development of compounds for the treatment of drug abuse and its consequences.

1.本合同向NIDA治疗和医学后果司提供报告，其中承包商通过对大量 生物靶标。 2.本合同还将支持进行研究，以确定测试化合物对化合物图谱或其他来源所示特定生物目标的受体的亲和力(IC50，KI)和/或功能(EC50，IC50)。 3.这项合同将提供一种方法，在一个或多个受体或转运体上筛选更多化合物，可能是大型化合物库，以确定生物活性，目的是发现具有新化学结构的特定受体或转运体配体。 4.该合同将提供测试，以评估关键领域的预测毒理学，这些领域可能表明一种候选化合物在药物开发过程中会遇到困难。 5.本合同将允许对可能在开发治疗药物滥用及其后果的化合物方面具有重要意义的目标进行体外分析。